441 articles for thisTarget
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Article Title
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Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
Shanghai Institute of Materia Medica
New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
University of Bari Aldo Moro
Importance of 5/6-aryl substitution on the pharmacological profile of 4'-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid derived PPAR¿ agonists.
University of Innsbruck
Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of novel quinoxaline derivatives as potential PPAR¿ and SUR agonists.
Al-Azhar University
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Evaluation of selected 3D virtual screening tools for the prospective identification of peroxisome proliferator-activated receptor (PPAR)¿ partial agonists.
University of Innsbruck
New telmisartan-derived PPAR¿ agonists: Impact of the 3D-binding mode on the pharmacological profile.
Universit£T Innsbruck
Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists.
Galderma R & D
Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptora/d (PPARa/d) dual agonistic activity.
The University of Tokyo
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.
Bristol-Myers Squibb
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.
Central Pharmaceutical Research Institute
Amorfrutin C Induces Apoptosis and Inhibits Proliferation in Colon Cancer Cells through Targeting Mitochondria.
Max Planck Institute For Molecular Genetics
N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor¿ Modulators.
Goethe-University Frankfurt
Design and synthesis of novel Y-shaped barbituric acid derivatives as PPAR¿ activators.
National Institute of Pharmaceutical Education and Research (NIPER)
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3.
Pfizer
Novel Oxazolidinone-Based Peroxisome Proliferator Activated Receptor Agonists: Molecular Modeling, Synthesis, and Biological Evaluation.
IQM-CSIC
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Genentech
Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor¿/d agonists.
Sookmyung Women'S University
Anthranilic acid derivatives as nuclear receptor modulators--development of novel PPAR selective and dual PPAR/FXR ligands.
Goethe-University Frankfurt
2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPAR¿ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes.
University of Copenhagen
Amorfrutins Are Natural PPAR¿ Agonists with Potent Anti-inflammatory Properties.
Max Planck Institute For Molecular Genetics
Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.
Punjabi University
Peroxisome Proliferator-Activated Receptor¿ (PPAR¿) and Ligand Choreography: Newcomers Take the Stage.
Universitat Rovira I Virgili (Urv)
Separation and peroxisome proliferator-activated receptor-¿ agonist activity evaluation of synthetic racemic bavachinin enantiomers.
Shanghai University of Traditional Chinese Medicine
Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARa/¿ agonists.
Bristol-Myers Squibb Research and Development (R & D)
SAR-studies of¿-secretase modulators with PPAR¿-agonistic and 5-lipoxygenase-inhibitory activity for Alzheimer's disease.
Goethe-University Frankfurt
Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptora/¿ ligand LT175.
University of Bari Aldo Moro
Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARa/¿ activation and dual 5-LO/mPGES-1 inhibition.
Goethe-University Frankfurt
Molecular determinants for improved activity at PPARa: structure-activity relationship of pirinixic acid derivatives, docking study and site-directed mutagenesis of PPARa.
Goethe-University Frankfurt
Molecular dynamics study-guided identification of cyclic amine structures as novel hydrophobic tail components of hPPAR¿ agonists.
Okayama University
Bioactive diterpenoids and flavonoids from the aerial parts of Scoparia dulcis.
Institute of Chinese Materia Medica
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Biological evaluation and structural insights for design of subtype-selective peroxisome proliferator activated receptor-a (PPAR-a) agonists.
National Institute of Pharmaceutical Education and Research (NIPER)
Structural development studies of PPARs ligands based on tyrosine scaffold.
Universit£&Quot;G. D'Annunzio&Quot
Polyyne hybrid compounds from Notopterygium incisum with peroxisome proliferator-activated receptor gamma agonistic effects.
Karl-Franzens-University Graz
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Extending the structure-activity relationship of anthranilic acid derivatives as farnesoid X receptor modulators: development of a highly potent partial farnesoid X receptor agonist.
Goethe-University Frankfurt
The dipeptide H-Trp-Glu-OH (WE) shows agonistic activity to peroxisome proliferator-activated protein-a and reduces hepatic lipid accumulation in lipid-loaded H4IIE cells.
Korea University
Identification of the first potent, selective and bioavailable PPARa antagonist.
Inception Sciences
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
Glaxo Wellcome Research and Development
Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPAR¿ agonists.
Glaxosmithkline
Discovery of INT131: a selective PPAR¿ modulator that enhances insulin sensitivity.
Amgen
Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor¿.
Helmholtz Centre For Infection Research
The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.
The University of Sydney
Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-¿.
Pfizer
New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptora/¿ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression.
Universit�
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.
Glaxosmithkline
QSAR analysis of PPAR-gamma agonists as anti-diabetic agents.
Central Drug Research Institute
Phenoxyacetic acids as PPARd partial agonists: synthesis, optimization, and in vivo efficacy.
Glaxosmithkline
Flexible ligand recognition of peroxisome proliferator-activated receptor-gamma (PPARgamma).
Rikkyo University
Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.
Glaxosmithkline
Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs.
D'Annunzio University of Chieti
Design, synthesis and evaluation of novel zwitterionic compounds as PPARa/¿ dual agonists (1).
Daiichi Sankyo
Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
Istituto Tumori&Quot;Giovanni Paolo Ii&Quot
Design and synthesis of dual modulators of soluble epoxide hydrolase and peroxisome proliferator-activated receptors.
Zafes/Liff/Osf Goethe-University Frankfurt
Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor¿.
University of Naples Federico II
Sesquiterpene lactones from Tithonia diversifolia act as peroxisome proliferator-activated receptor agonists.
National Kaohsiung Normal University
Diarylheptanoid glycosides from Tacca plantaginea and their effects on NF-¿B activation and PPAR transcriptional activity.
Chungnam National University
Design, synthesis and in vitro evaluation of a series ofa-substituted phenylpropanoic acid PPAR¿ agonists to further investigate the stereochemistry-activity relationship.
Okayama University
Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.
University of Innsbruck
Synthesis and evaluation of sulfonylnitrophenylthiazoles (SNPTs) as thyroid hormone receptor-coactivator interaction inhibitors.
Institut Pasteur Korea
Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators.
University of Lille Nord de France
Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
Trinity College
Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPAR¿ modulators.
Daiichi Sankyo
Activity landscape modeling of PPAR ligands with dual-activity difference maps.
Universidad Nacional Aut£Noma De M£Xico
Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptord agonists as potent anti-obesity agents in vivo.
Seoul National University
Polyhydroxylated macrolides from Seimatosporium discosioides and their effects on the activation of peroxisome proliferator-activated receptor gamma.
Korea University
Total synthesis and dual PPARa/¿ agonist effects of amorphastilbol and its synthetic derivatives.
Korea Institute of Science and Technology
Structure-activity relationships and key structural feature of pyridyloxybenzene-acylsulfonamides as new, potent, and selective peroxisome proliferator-activated receptor (PPAR)¿ Agonists.
Takeda Pharmaceutical
Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldii.
Chungnam National University
Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents.
Johnson & Johnson Pharmaceutical Research and Development
Design, synthesis, and structural analysis of phenylpropanoic acid-type PPAR¿-selective agonists: discovery of reversed stereochemistry-activity relationship.
Okayama University
Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazone.
Kyorin Pharmaceutical
(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
Institute of Pharmacology and Toxicology
Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.
Daiichi Sankyo
Identification of (beta-carboxyethyl)-rhodanine derivatives exhibiting peroxisome proliferator-activated receptor gamma activity.
Sookmyung Women'S University
Acidic elements in histamine H(3) receptor antagonists.
Johann Wolfgang Goethe University
Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
Chinese Academy of Sciences
Tryptophan-containing dipeptide derivatives as potent PPARgamma antagonists: design, synthesis, biological evaluation, and molecular modeling.
Graduate School of The Chinese Academy of Sciences
Modulation of PPAR receptor subtype selectivity of the ligands: aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety.
Zydus Research Centre
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
Seoul National University
Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.
Bristol-Myers Squibb R & D
Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.
Usda-Ars
Comparative metabolism of radiolabeled muraglitazar in animals and humans by quantitative and qualitative metabolite profiling.
Bristol-Myers Squibb
Synthesis and structure-activity relationships of thiadiazole-derivatives as potent and orally active peroxisome proliferator-activated receptors alpha/delta dual agonists.
Johnson & Johnson Pharmaceutical Research and Development
Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.
Nippon Shinyaku
SAR-oriented discovery of peroxisome proliferator-activated receptor pan agonist with a 4-adamantylphenyl group as a hydrophobic tail.
University of Tokyo
Discovery of a novel class of 1,3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.
Nippon Shinyaku
Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
Central Drug Research Institute
Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
Bristol-Myers Squibb Research and Development
Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.
Johnson & Johnson
Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARgamma ligands (I).
Fudan University
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
Eli Lilly
Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.
University of Mississippi
O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.
Merck Research Laboratories
Novel oximes having 5-benzyl-2,4-thiazolidinedione as antihyperglycemic agents: synthesis and structure-activity relationship.
Sankyo
Acetylenic acid analogues from the edible mushroom Chanterelle (Cantharellus cibarius) and their effects on the gene expression of peroxisome proliferator-activated receptor-gamma target genes.
Korea University
Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptorsa/¿ dual agonists.
University of Bari Aldo Moro
Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPAR¿ partial agonists.
Daiichi Sankyo
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor¿ (PPAR¿) modulators.
Merck Research Laboratories
A new class of non-thiazolidinedione, non-carboxylic-acid-based highly selective peroxisome proliferator-activated receptor (PPAR)¿ agonists: design and synthesis of benzylpyrazole acylsulfonamides.
Takeda Pharmaceutical
Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor¿ selective agonists with protein-tyrosine phosphatase 1B inhibition.
Kyoto Pharmaceutical Industries
Discovery of cyclic amine-substituted benzoic acids as PPARa agonists.
Kyorin Pharmaceutical
Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.
University of Oslo
Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: relationship between absolute configuration and subtype selectivity.
The University of Tokyo
Revisiting glitazars: thiophene substituted oxazole containinga-ethoxy phenylpropanoic acid derivatives as highly potent PPARa/¿ dual agonists devoid of adverse effects in rodents.
Zydus Research Centre
Novel thiazolidinedione derivatives with anti-obesity effects: dual action as PTP1B inhibitors and PPAR-¿ activators.
Inha University
Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-¿.
Pfizer
Discovery of new nanomolar peroxisome proliferator-activated receptor κ activators via elaborate ligand-based modeling.
Universiti Sains Malaysia
Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.
Guiyang Medical College
Structure-based design, synthesis, and nonalcoholic steatohepatitis (NASH)-preventive effect of phenylpropanoic acid peroxisome proliferator-activated receptor (PPAR)a-selective agonists.
Okayama University
Biological evaluation of novel benzisoxazole derivatives as PPARd agonists.
Nippon Chemiphar
Structural requirements of flavonoids for the adipogenesis of 3T3-L1 cells.
Kyoto Pharmaceutical University
Synthesis and pharmacological evaluation of novel benzoylazole-based PPARa/κ activators.
Dainippon Sumitomo Pharma
Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARd agonists.
Astrazeneca R&D Charnwood
Development of a new class of benzoylpyrrole-based PPARa/¿ activators.
Dainippon Sumitomo Pharma
Synthesis of a novel human PPARd selective agonist and its stimulatory effect on oligodendrocyte differentiation.
Nippon Chemiphar
Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.
Zydus Research Centre
Selective peroxisome proliferator-activated receptord isosteric selenium agonists as potent anti-atherogenic agents in vivo.
Seoul National University
1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPAR¿ partial agonists.
Sookmyung Women'S University
Characterization of new PPARgamma agonists: benzimidazole derivatives-importance of positions 5 and 6, and computational studies on the binding mode.
Freie UniversitäT Berlin
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.
Zafes/Liff/Goethe University Frankfurt
Synthesis and anti-inflammatory activity of new arylidene-thiazolidine-2,4-diones as PPARgamma ligands.
Universidade Federal De Pernambuco
Synthesis and structure-activity relationships of 2-aryl-4-oxazolylmethoxy benzylglycines and 2-aryl-4-thiazolylmethoxy benzylglycines as novel, potent PPARalpha selective activators- PPARalpha and PPARgamma selectivity modulation.
Bristol-Myers Squibb R & D
Truxillic acid derivatives act as peroxisome proliferator-activated receptor gamma activators.
Goethe-University Frankfurt
Rational design of a pirinixic acid derivative that acts as subtype-selective PPARgamma modulator.
Goethe-University Frankfurt
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).
Bristol-Myers Squibb
Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists.
The Genomics Institute of The Novartis Research Foundation
Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) delta selective antagonists.
The University of Tokyo
Design and synthesis of novel bis-oximinoalkanoic acids as potent PPARalpha agonists.
Zydus Research Centre
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.
Glaxosmithkline
7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.
The University of Sydney
New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.
University of Bari Aldo Moro
Discovery of a novel class of 2-mercaptohexanoic acid derivatives as highly active PPARalpha agonists.
Goethe-University Frankfurt
Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
Wake Forest University
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
Umr Gicc
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
Merck Research Laboratories
Non thiazolidinedione antihyperglycaemic agents. 2: α-Carbon substituted β-phenylpropanoic acids1
TBA
Non thiazolidinedione antihyperglycaemic agents. 1: α-Heteroatom substituted β-phenylpropanoic acids
TBA
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma a
Merck Research Laboratories
Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
F. Hoffmann-La Roche
Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
National Health Research Institutes
Selective, potent PPARgamma agonists with cyclopentenone core structure.
Universidade De Vigo
Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.
Bristol-Myers Squibb Research and Development
Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.
Università
Discovery of novel PPAR ligands by a virtual screening approach based on pharmacophore modeling, 3D shape, and electrostatic similarity screening.
University of Innsbruck
Analogues of 2-phenyl-ethenesulfonic acid phenyl ester have dual functions of inhibiting expression of inducible nitric oxide synthase and activating peroxisome proliferator-activated receptor gamma.
National Health Research Institutes
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
Zydus Research Centre
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
Yuhan Research Institute
New PPARgamma ligands based on barbituric acid: virtual screening, synthesis and receptor binding studies.
National Institute of Pharmaceutical Education and Research
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Sulindac derivatives that activate the peroxisome proliferator-activated receptor gamma but lack cyclooxygenase inhibition.
Vanderbilt University Center For Structural Biology
Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: effect of introduction of fluorine at the linker part.
The University of Tokyo
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
Zydus Research Centre
New PPARgamma ligands based on 2-hydroxy-1,4-naphthoquinone: computer-aided design, synthesis, and receptor-binding studies.
National Institute of Pharmaceutical Education and Research
Effects of amide constituents from pepper on adipogenesis in 3T3-L1 cells.
Kyoto Pharmaceutical University
Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.
Graduate School of The Chinese Academy of Sciences
CoMFA analysis of dual/multiple PPAR activators.
National Institute of Pharmaceutical Education and Research
Bioassay for the identification of natural product-based activators of peroxisome proliferator-activated receptor-gamma (PPARgamma): the marine sponge metabolite psammaplin A activates PPARgamma and induces apoptosis in human breast tumor cells.
University of Mississippi
Two new furanoditerpenes from Saururus chinenesis and their effects on the activation of peroxisome proliferator-activated receptor gamma.
Korea Research Institute of Bioscience and Biotechnology
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
Spot-Ea3857
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.
Glaxosmithkline
Chlorocyclinones A-D, chlorinated angucyclinones from Streptomyces sp. strongly antagonizing rosiglitazone-induced PPAR-gamma activation.
Boehringer Ingelheim Pharma
Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
Eli Lilly
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
Wyeth Pharmaceuticals
Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor gamma (PPARgamma) agonists.
Korea Research Institute of Chemical Technology
Discovery of PPARγ and glucocorticoid receptor dual agonists to promote the adiponectin and leptin biosynthesis in human bone marrow mesenchymal stem cells.
Seoul National University
Discovery of a structurally novel, potent, and once-weekly free fatty acid receptor 1 agonist for the treatment of diabetes.
Guangdong Pharmaceutical University
Development of a Potent Nurr1 Agonist Tool for In Vivo Applications.
Ludwig Maximilian University of Munich
Structure-Activity Relationships of Truncated 1'-Homologated Carbaadenosine Derivatives as New PPARγ/δ Ligands: A Study on Sugar Puckering Affecting Binding to PPARs.
Seoul National University
Design and synthesis of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid derivatives as PPARgamma activators.
National Institute of Pharmaceutical Education and Research
Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
Re&D Vufb
Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.
Kowa
Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) delta-selective agonists.
University of Tokyo
Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists.
Nagoya City University
Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.
Johnson and Johnson Pharmaceutical Research and Development
Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists.
Pfizer
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
Seoul National University
Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) delta agonists.
Pfizer
Design, synthesis, and biological evaluation of deuterated indolepropionic acid derivatives as novel long-acting pan PPARα/γ/δ agonists.
Guangdong Pharmaceutical University
Discovery of orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid.
Soochow University
Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
Novo Nordisk
Discovery of the First Subnanomolar PPARα/δ Dual Agonist for the Treatment of Cholestatic Liver Diseases.
China Pharmaceutical University
Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.
Guangdong Pharmaceutical University
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, Synthesis, and Anti-Inflammatory Evaluation of a Novel PPARδ Agonist with a 4-(1-Pyrrolidinyl)piperidine Structure.
Shionogi
Discovery and structure-activity relationship study of 2-piperazinyl-benzothiazole derivatives as potent and selective PPARδ agonists.
Shionogi
Emerging targets and potential therapeutic agents in non-alcoholic fatty liver disease treatment.
Sichuan University
Therapeutic journey of 2,4-thiazolidinediones as a versatile scaffold: An insight into structure activity relationship.
Jamia Hamdard
Thiazolidinediones and PPAR orchestra as antidiabetic agents: From past to present.
Birla Institute of Technology
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.
Bristol Myers Squibb
Prenylated Chrysin Derivatives as Partial PPARγ Agonists with Adiponectin Secretion-Inducing Activity.
Seoul National University
Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups--new classes of PPAR gamma/delta and PPAR alpha/gamma/delta agonists.
Bayer Pharmaceuticals
Aldose reductase and protein tyrosine phosphatase 1B inhibitors as a promising therapeutic approach for diabetes mellitus.
Aristotle University of Thessaloniki
Novel linked butanolide dimer compounds increase adiponectin production during adipogenesis in human mesenchymal stem cells through peroxisome proliferator-activated receptor γ modulation.
Seoul National University
Natural products and analogs as preventive agents for metabolic syndrome via peroxisome proliferator-activated receptors: An overview.
University Clinic Hospital of Valencia
Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Institute of Mit and Harvard
Design, synthesis and biological evaluation of cajanonic acid A analogues as potent PPAR γ antagonists.
Guizhou Medical University
Bioactive Aurones, Indanones, and Other Hemiindigoid Scaffolds: Medicinal Chemistry and Photopharmacology Perspectives.
Universite Grenoble Alpes
Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.
National Health Research Institutes
Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
Eli Lilly
Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
Pfizer
Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
Pfizer
Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
Eli Lilly
Alkaloids and Coumarins with Adiponectin-Secretion-Promoting Activities from the Leaves of
Seoul National University
Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis.
Procter and Gamble Pharmaceuticals
Indenone derivatives: a novel template for peroxisome proliferator-activated receptor gamma (PPARgamma) agonists.
Korea Research Institute of Chemical Technology
Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus,
Seoul National University
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.
The Genomics Institute of The Novartis Research Foundation
Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists.
F. Hoffmann-La Roche
Discovery of a Novel Class of d-Amino Acid Oxidase Inhibitors Using the Schrödinger Computational Platform.
Schr£Dinger
Structure-based drug design of a novel family of PPARgamma partial agonists: virtual screening, X-ray crystallography, and in vitro/in vivo biological activities.
National Health Research Institutes
A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
Universit£?Degli Studi Di Bari "Aldo Moro
Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
University of Toronto
1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.
The Genomics Institute of The Novartis Research Foundation
Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.
Guangdong Pharmaceutical University
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis.
Southern Medical University Biomedical Research Center
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
Guangdong Pharmaceutical University
Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.
National Health Research Institutes
Design and synthesis of potent and subtype-selective PPARalpha agonists.
Merck Research Laboratories
Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.
National Health Research Institutes
Design and synthesis of substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor alpha/delta dual agonists.
University of Tokyo
Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton.
Northwest University
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Merck Research Laboratories
Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
Cnrs Umr 6052
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.
Merck Research Laboratories
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.
Università
Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method.
Shionogi
Structure-Activity Relationship Studies of Trisubstituted Isoxazoles as Selective Allosteric Ligands for the Retinoic-Acid-Receptor-Related Orphan Receptor γt.
Technische Universiteit Eindhoven
Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
Eindhoven University of Technology
Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
Merck Research Laboratories
(2R)-2-methylchromane-2-carboxylic acids: discovery of selective PPARalpha agonists as hypolipidemic agents.
Merck Research Laboratories
The evolution paths of some reprehensive scaffolds of RORγt modulators, a perspective from medicinal chemistry.
Sun Yat-Sen University
Design, Synthesis, and Biological Activity of l-1'-Homologated Adenosine Derivatives.
Chonnam National University
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Galangin 3-benzyl-5-methylether derivatives function as an adiponectin synthesis-promoting peroxisome proliferator-activated receptor γ partial agonist.
Seoul National University
Selective PPARgamma modulators with improved pharmacological profiles.
Merck Research Laboratories
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
Merck Research Laboratories
Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists
Broad Institute of Mit and Harvard
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
Bristol-Myers Squibb Pharmaceutical Research Institute
FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity.
University of Siena
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
Eli Lilly
Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors.
Goethe-University
Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
Astrazeneca
Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis.
China Pharmaceutical University
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.
Goethe University
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Glaxosmithkline
Thiazolidinedione "Magic Bullets" Simultaneously Targeting PPARγ and HDACs: Design, Synthesis, and Investigations of their
Bharati Vidyapeeth'S College of Pharmacy
A Photohormone for Light-Dependent Control of PPARα in Live Cells.
Goethe-University Frankfurt
Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Their Common Age-Related Comorbidities.
Albany College of Pharmacy and Health Sciences
Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
Research Institute of Tsinghua University
Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
University of Toledo College of Pharmacy and Pharmaceutical Sciences
(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
Merck Research Laboratories
Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists.
Eli Lilly
Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
Guangdong Pharmaceutical University
Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.
Xiamen University
Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.
Johnson and Johnson Pharmaceutical Research and Development
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Virtual screening and biological evaluation of PPARγ antagonists as potential anti-prostate cancer agents.
University of Nebraska Medical Center
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
Eli Lilly
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Ligand Pharmaceuticals
Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
Novo Nordisk
Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists.
Merck Research Laboratories
Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Ligand Pharmaceuticals
Discovery of novel modulators for the PPARα (peroxisome proliferator activated receptor α): Potential therapies for nonalcoholic fatty liver disease.
City of Hope National Medical Center
Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
China Pharmaceutical University
Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor alpha subtype-selective activators.
Kyorin Pharmaceutical
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
Merck Research Laboratories
Structure-Activity Relationship Study and Biological Evaluation of 2-(Disubstituted phenyl)-indole-5-propanoic Acid Derivatives as GPR40 Full Agonists.
Sungkyunkwan University
Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells.
University of Innsbruck
5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
Merck Research Laboratories
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
Glaxosmithkline
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
Novo Nordisk
Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
Merck Research Laboratories
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
Novo Nordisk
Synthesis and pharmacological evaluation of a new class of peroxisome proliferator-activated receptor modulators.
Biovitrum
Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD).
Mitobridge
Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
University of Oslo
Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities.
Chongqing Medical University
Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators.
Seoul National University
A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor γ Binding Properties and Biological Activities.
Aix Marseille University
Discovery of Bispecific Antagonists of Retinol Binding Protein 4 That Stabilize Transthyretin Tetramers: Scaffolding Hopping, Optimization, and Preclinical Pharmacological Evaluation as a Potential Therapy for Two Common Age-Related Comorbidities.
Albany College of Pharmacy and Health Sciences
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Tes Pharma
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
Novo Nordisk
Enantio-dependent binding and transactivation of optically active phenylpropanoic acid derivatives at human peroxisome proliferator-activated receptor alpha.
Kyorin Pharmaceutical
Kojyl cinnamate esters are peroxisome proliferator-activated receptor α/γ dual agonists.
Seoul National University
Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators.
Kyorin Pharmaceutical
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Glaxosmithkline
Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor γ (PPARγ).
New York University
Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis.
Glaxosmithkline
2-Phenyl-8-(1-phenylallyl)-chromenone compounds have a pan-PPAR modulator pharmacophore.
Seoul National University
Structure-Activity Relationship Studies of 3- or 4-Pyridine Derivatives of DS-6930.
Daiichi Sankyo
Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta.
Glaxosmithkline
l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
Goethe-University Frankfurt
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
Eli Lilly
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.
Glaxosmithkline
Sulfonimide and Amide Derivatives as Novel PPARα Antagonists: Synthesis, Antiproliferative Activity, and Docking Studies.
"G. D'Annunzio" University of Chieti-Pescara
Addressing hERG activity while maintaining favorable potency, selectivity and pharmacokinetic properties of PPARδ modulators.
Mitobridge
Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ.
Seoul National University
Discovery of Second Generation RORγ Inhibitors Composed of an Azole Scaffold.
Kyoto Prefectural University of Medicine
Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes.
Boryung Pharmaceuticals
Novel Phenyldiazenyl Fibrate Analogues as PPAR α/γ/δ Pan-Agonists for the Amelioration of Metabolic Syndrome.
University of Chieti "G. D.Annunzio
Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
The University of Tokyo
Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.
Guangdong Pharmaceutical University
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
Goethe University Frankfurt
Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone.
The Scripps Research Institute
The PPARs: from orphan receptors to drug discovery.
Glaxo Wellcome Research & Development
Novel berberine-based derivatives with potent hypoglycemic activity.
Guizhou Medical University
Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.
Glaxo Wellcome Research and Development
Role of sulphur-heterocycles in medicinal chemistry: An update.
Maharaja Ranjit Singh Punjab Technical University
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute of The Novartis Research Foundation (Gnf)
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.
Glaxo Wellcome Research & Development
Novel thiazolidines: Synthesis, antiproliferative properties and 2D-QSAR studies.
University of Texas-Arlington
An update about the crucial role of stereochemistry on the effects of Peroxisome Proliferator-Activated Receptor ligands.
University of Bari Aldo Moro
Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
University of Oslo
Structure-activity relationship and synthetic methodologies of α-santonin derivatives with diverse bioactivities: A mini-review.
Shanghai Ocean University
Structural development of 1H-pyrazolo-[3,4-b]pyridine-4-carboxylic acid derivatives as human peroxisome proliferator-activated receptor alpha (PPARα)-selective agonists.
Okayama University
(3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents.
Kyorin Pharmaceutical
Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists.
Technische Universiteit Eindhoven
Differential activity of rosiglitazone enantiomers at PPAR gamma.
Glaxo Wellcome Research and Development
Overcoming imatinib resistance in chronic myelogenous leukemia cells using non-cytotoxic cell death modulators.
University of Innsbruck
Structure optimization of a new class of PPARγ antagonists.
Fraunhofer Institute For Molecular Biology and Applied Ecology Ime
Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.
The University of Oklahoma Health Science Center
A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
Goethe-University Frankfurt
Multitarget PPARγ agonists as innovative modulators of the metabolic syndrome.
University of Chieti "G. D.Annunzio
Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders.
University of Oklahoma
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
Terns Pharmaceuticals
Polycerasoidol, a Natural Prenylated Benzopyran with a Dual PPARα/PPARγ Agonist Activity and Anti-inflammatory Effect.
University of Valencia
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as ROR��t Allosteric Inhibitors for Autoimmune Diseases
Merck
Adiponectin-Secretion-Promoting Phenylethylchromones from the Agarwood of Aquilaria malaccensis.
Seoul National University
Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.
Inception Sciences
Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.
Boryung Pharmaceuticals
Mechanistic Insight on the Mode of Action of Colletoic Acid.
The University of Tennessee Health Science Center
Development of a novel class of peroxisome proliferator-activated receptor (PPAR) gamma ligands as an anticancer agent with a unique binding mode based on a non-thiazolidinedione scaffold.
Hokkaido University
Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist for the Treatment of Primary Biliary Cirrhosis.
Wuxi Apptec (Shanghai) Co.
Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo.
Ume£
Identification of dual PPARα/γ agonists and their effects on lipid metabolism.
The University of Sydney
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.
Glaxo Wellcome Research and Development
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
University of Cagliari
Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.
The Scripps Research Institute
Adipogenetic effects of retrofractamide A derivatives in 3T3-L1 cells.
Kyoto Pharmaceutical University
Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.
University of Bari Aldo Moro
Design and synthesis of a series of α-benzyl phenylpropanoic acid-type peroxisome proliferator-activated receptor (PPAR) gamma partial agonists with improved aqueous solubility.
Okayama University
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.
Glaxo Wellcome Research and Development
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety.
Glaxo Wellcome Research and Development
Development of Dihydrodibenzooxepine Peroxisome Proliferator-Activated Receptor (PPAR) Gamma Ligands of a Novel Binding Mode as Anticancer Agents: Effective Mimicry of Chiral Structures by Olefinic E/ Z-Isomers.
Fuji Research Park, R&D Division
Stereoselective Synthesis of the Isomers of Notoincisol A: Assigment of the Absolute Configuration of this Natural Product and Biological Evaluation.
Vienna University of Technology
Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
Guangdong Pharmaceutical University
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
Boryung Pharmaceuticals
PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.
Sptanis Pharmachem Consulting
Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
Goethe University Frankfurt
Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
University of Bari Aldo Moro
Synthesis and evaluation of an orally available "Y"-shaped biaryl peroxisome proliferator-activated receptor δ agonist.
Daegu-Gyeongbuk Medical Innovation Foundation
Design, synthesis, and evaluation of novel l-phenylglycine derivatives as potential PPARγ lead compounds.
Southwest University
Structure-guided evolution of a 2-phenyl-4-carboxyquinoline chemotype into PPARα selective agonists: New leads for oculovascular conditions.
University of Oklahoma
A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies.
Shenyang Pharmaceutical University
2-Formyl-komarovicine promotes adiponectin production in human mesenchymal stem cells through PPARγ partial agonism.
Seoul National University
Novel highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulators with pharmacokinetic properties suitable for once-daily oral dosing.
Mitobridge
Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
Daiichi Sankyo
Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
Daiichi Sankyo
Synthesis and biological evaluation of novel bavachinin analogs as anticancer agents.
Csir-Indian Institute of Integrative Medicine
SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.
Sungkyunkwan University
Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
University of Lille
Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
Janssen Research and Development
Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-γ/FFAR1 agonists.
Suez Canal University
Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of quinazolin-4(3H)-one derivatives as potential PPARγ and SUR agonists.
Al-Azhar University
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.
Bristol-Myers Squibb
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR)α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
Inventiva
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Bristol-Myers Squibb
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptorα/δ (PPARα/δ) dual agonists.
The University of Tokyo
Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.
The University of Tokyo
A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase To Counter Nonalcoholic Steatohepatitis.
Goethe-University Frankfurt
Structure-Activity Relationship of 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide (INT131) Analogs for PPARγ-Targeted Antidiabetics.
The Scripps Research Institute
Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment
Clavius Pharmaceuticals
Substituted acethydrazide derivative, preparation method and use thereof
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases
Universite De Lille 2 Droit Et Sante
2-aryl- and 2-arylalkyl-benzimidazoles as mIDH1 inhibitors
Bayer Pharma Aktiengesellschaft
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinase (ROCK) and methods of use
H. Lee Moffitt Cancer Center and Research Institute
Heterocyclic derivatives and their use in the treatment of neurological disorders
Novartis
[35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents.
Institut De Recherches Servier
Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies.
Gliatech
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
University of Tokyo
2H-Thieno[3,2-e]- and [2,3-e]-1,2-thiazine-6-sulfonamide 1,1-dioxides as ocular hypotensive agents: synthesis, carbonic anhydrase inhibition and evaluation in the rabbit.
Alcon Research