154 articles for thisTarget
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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
Exploring new scaffolds for angiotensin II receptor antagonism.
National Hellenic Research Foundation
Mimicking of Arginine by Functionalized N(¿)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
University of Regensburg
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
Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands.
Uppsala University
Optimized protein kinase C¿ (PKC¿) inhibitors reveal only modest anti-inflammatory efficacy in a rodent model of arthritis.
Abbvie Bioresearch Center
Structure-activity relationship studies toward the discovery of selective apelin receptor agonists.
University of Strasburg
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
NO-sartans: a new class of pharmacodynamic hybrids as cardiovascular drugs.
University of Pisa
The replacement of His(4) in angiotensin IV by conformationally constrained residues provides highly potent and selective analogues.
Vrije Universiteit Brussel
Synthesis and In Vitro evaluation of fused ring heterocyle-containing angiotensin II antagonists.
TBA
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research and Development
Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.
Sanford-Burnham Medical Research Institute
The discovery of new potent non-peptide Angiotensin II AT1 receptor blockers: a concise synthesis, molecular docking studies and biological evaluation of N-substituted 5-butylimidazole derivatives.
University of Patras
Design, synthesis and biological activity of 6-substituted carbamoyl benzimidazoles as new nonpeptidic angiotensin II AT1 receptor antagonists.
School of Chemical Engineering & The Environment
Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.
China Pharmaceutical University
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Selective angiotensin II AT(2) receptor agonists with reduced CYP 450 inhibition.
Uppsala University
Design, synthesis, and biological evaluation of AT1 angiotensin II receptor antagonists based on the pyrazolo[3,4-b]pyridine and related heteroaromatic bicyclic systems.
University of Siena
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
Technische Universit£T Darmstadt
Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.
Neogenesis
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
Dupont Pharmaceuticals
Novel cyclic analogs of angiotensin II with cyclization between positions 5 and 7: conformational and biological implications.
Washington University
Nonpeptide angiotensin II receptor antagonists. Synthesis and biological activity of benzimidazolecarboxylic acids.
Takeda Chemical Industries
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
Kyung Hee University
Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazole derivatives as nonpeptidic angiotensin II AT1 receptor antagonists.
Beijing Institute of Technology
Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation.
University of Lille
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
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
The M. S. University of Baroda
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Universite De Sherbrooke
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.
Glaxosmithkline
The design, binding affinity prediction and synthesis of macrocyclic angiotensin II AT1 and AT2 receptor antagonists
TBA
L-162,389: a potent orally active angiotensin II receptor antagonist with balanced affinity to both AT1 and AT2 receptor subtypes
TBA
AT1 selective angiotensin II antagonists with phenoxyphenylacetic acid as a biphenyl replacement part I
TBA
The SAR of 6-(N-alkyl-N-acyl)-2-propyl-3-[(2′-tetrazol-5-yl)biphen-4-yl)methyl]-quinazolinones as balanced affinity antagonists of the human AT1 and AT2 receptors
TBA
α-Phenoxyphenylacetic acid derived angiotensin II antagonists with low nanomolar AT1/AT2 receptor subtype affinity (Part II)
TBA
Substituted 1,3-benzodioxole & 1,3-benzodithiole -2- carboxylates and their tetrazole analogs with potent binding affinity to the angiotensin II AT1 receptor
TBA
Potent triazolinone-based angiotensin II receptor antagonists with equivalent affinity for both the AT1 and AT2 subtypes
TBA
The synthesis and biological activity of tetrahydroquinoline angiotensin II antagonists containing a substituted biphenyltetrazole group
TBA
Development of angiotensin II antagonists with equipotent affinity for human AT1 and AT2 receptor subtypes.
TBA
Balanced angiotensin II receptor antagonists. III. The effects of substitution at the imidazole 5-position.
TBA
Balanced angiotensin II receptor antagonists. II.1,2 4-aminomethyl- and acylaminomethylimidazoles
TBA
Synthesis and biological evaluation of the potent isoxazolidinyl angiotensin II receptor antagonist CL332,877 and its enantiomers.
TBA
6-isoxazolinyl and isoxazolidinyl substituted quinazolinones as angiotensin II receptor antagonists
TBA
A new class of balanced AT1/AT2 angiotensin II antagonists: quinazolinone AII antagonists with acylsulfonamide and sulfonylcarbamate acidic functionalities
TBA
Quinazolinone Biphenyl Acylsulfonamides: A potent new class of angiotensin-II receptor antagonists
TBA
Potent imidazole angiotensinII antagonists: acyl sulfonamides and acyl sulfamides as tetrazole replacements
TBA
Evaluation of heterocyclic acid equivalents as tetrazole replacements in imidazopyridine-based nonpeptide angiotensin II receptor antagonists
TBA
Valsartan, a potent, orally active angiotensin II antagonist developed from the structurally new amino acid series
TBA
Synthesis of new imidazo[1,2-b]pyridazine isosteres of potent imidazo[4,5-b]pyridine angiotensin II antagonists
TBA
Subtituted phenylthiophene benzoylsulfonamides with potent binding affinity to angiotensin II AT1 and AT2 receptors
TBA
Angiotensin II receptor antagonists: imidazoles and pyrroles bearing hydroxymethyl and carboxy substituents
TBA
New non-peptide angiotensin II receptor antagonists. 2: structure - activity relationship of a series of annelated 2(1H)-pyridinones
TBA
Triazolinones as nonpeptide angiotensin II antagonists. 2. discovery of a potent and orally active triazolinone acylsulfonamide
TBA
Quinazolinones 1: design and synthesis of potent quinazolinone- containing AT1-selective angiotensin-II receptor antagonists
TBA
Synthesis and structure-activity relationships of a novel series of non-peptide AT2-selective angiotensin II receptor antagonists
TBA
Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring.
Chinese Academy of Sciences
Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships.
Uppsala University
Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists.
China Pharmaceutical University
Synthesis and evaluation of imidazo[1,2-a]pyrazine derivatives as small molecule Gαq/11 inhibitors against uveal melanoma.
Sun Yat-Sen University
Design, synthesis and biological evaluation of novel indole-3-carboxylic acid derivatives with antihypertensive activity.
Lomonosov Moscow State University
Further studies on imidazo[4,5-b]pyridine AT1 angiotensin II receptor antagonists. Effects of the transformation of the 4-phenylquinoline backbone into 4-phenylisoquinolinone or 1-phenylindene scaffolds.
Università
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.
Tianjin University
2-Alkyl substituted benzimidazoles as a new class of selective AT2 receptor ligands.
Uppsala University
Quercetin derivatives: Drug design, development, and biological activities, a review.
Mazandaran University of Medical Sciences
Selective Discovery of GPCR Ligands within DNA-Encoded Chemical Libraries Derived from Natural Products: A Case Study on Antagonists of Angiotensin II Type I Receptor.
Northwest University
Discovery of Irbesartan Derivatives as BLT2 Agonists by Virtual Screening.
Fraunhofer Institute For Translational Medicine and Phamacology Itmp
Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice.
Rti International
Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability.
Vrije Universiteit Brussel
Comparison of 3D structures and AT(1) binding properties of pyrazolidine-3,5-diones and tetrahydropyridazine-3,6-diones with parent antihypertensive drug irbesartan.
Université
Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.
Wyeth Research
N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
Uppsala University
Identification of potent pyrazole based APELIN receptor (APJ) agonists.
Rti International
Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT(1) angiotensin II receptor antagonists.
Université
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
The Other Angiotensin II Receptor: AT
Centre Hospitalier Universitaire Vaudois (Chuv) and University of Lausanne (Unil
Multitarget PPARγ agonists as innovative modulators of the metabolic syndrome.
University of Chieti "G. D.Annunzio
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
Hydroxyl Groups in Synthetic and Natural-Product-Derived Therapeutics: A Perspective on a Common Functional Group.
University of Basel
Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
Sankyo
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
Discovery of novel, potent and low-toxicity angiotensin II receptor type 1 (AT1) blockers: Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazoles with a chiral center.
Beijing Institute of Technology
Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
Merck Research Laboratories
New nonpeptide angiotensin II receptor antagonists. 3. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)pyridine derivatives.
Zeneca Pharmaceuticals
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
Merck Research Laboratories
Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides.
Merck Research Laboratories
Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles.
Merck Research Laboratories
(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.
Merck Research Laboratories
Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
Merck Research Laboratories
A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor.
Merck Research Laboratories
Design, synthesis, and biological evaluation of 1,2,4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives as potential antihypertensive candidates.
China Pharmaceutical University
Triazolinone biphenylsulfonamide derivatives as orally active angiotensin II antagonists with potent AT1 receptor affinity and enhanced AT2 affinity.
Merck Research Laboratories
Nonpeptidic angiotensin II AT₁ receptor antagonists derived from 6-substituted aminocarbonyl and acylamino benzimidazoles.
Beijing Institute of Technology
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
Merck Research Laboratories
Triazolinone biphenylsulfonamides as angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes.
Merck Research Laboratories
Rational design, efficient syntheses and biological evaluation of N,N'-symmetrically bis-substituted butylimidazole analogs as a new class of potent Angiotensin II receptor blockers.
University of Patras
Novel angiotensin II receptor antagonists. Design, synthesis, and in vitro evaluation of dibenzo[a,d]cycloheptene and dibenzo[b,f]oxepin derivatives. Searching for bioisosteres of biphenylyltetrazole using a three-dimensional search technique.
Shionogi
Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes.
Merck Research Laboratories
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
Istituto Lusofarmaco
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.
Universitaire Vaudois
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
Boryung Pharmaceuticals
Integration of multi-scale molecular modeling approaches with experiments for the in silico guided design and discovery of novel hERG-Neutral antihypertensive oxazalone and imidazolone derivatives and analysis of their potential restrictive effects on cell proliferation.
Bahcesehir University (Bau)
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
New nonpeptide angiotensin II receptor antagonists. 2. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)quinoline derivatives.
Ici Pharmaceuticals Group
GLUN2B-SUBUNIT SELECTIVE ANTAGONISTS OF THE N-METHYL-D-ASPARTATE RECEPTORS WITH ENHANCED POTENCY AT ACIDIC PH
Emory University
COMPOSITIONS AND METHODS FOR ANTIOXIDANT AND ANTI-INFLAMMATORY THERAPEUTICS
Avanti Biosciences
Thermodynamics of hydrogen bond and hydrophobic interactions in cyclodextrin complexes.
Nih
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
Valeant Pharmaceuticals Research and Development