111 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
Design and Synthesis of Peptide YY Analogues with C-terminal Backbone Amide-to-Ester Modifications.
University of Copenhagen
Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.
University of Regensburg
Replacement of Thr32 and Gln34 in the C-terminal neuropeptide Y fragment 25-36 by cis-cyclobutane and cis-cyclopentane β-amino acids shifts selectivity toward the Y(4) receptor.
University of Regensburg
Heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 receptor antagonist.
Bristol-Myers Squibb Research and Development
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
University of Siena
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
Broad Institute of Mit and Harvard
Heterobivalent dual-target probe for targeting GRP and Y1 receptors on tumor cells.
The Ohio State University
Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists.
Glaxosmithkline
The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists.
Glaxosmithkline
Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists.
TBA
Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor.
Pfizer
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
Aska Pharmaceutical
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.
The University of Mississippi
Discovery of novel orally active ureido NPY Y5 receptor antagonists.
Schering-Plough Research Institute
Truncated, branched, and/or cyclic analogues of neuropeptide Y: importance of the pancreatic peptide fold in the design of specific Y2 receptor ligands.
Salk Institute
Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder.
Lundbeck Research Usa
Discovery of pyridone-containing imidazolines as potent and selective inhibitors of neuropeptide Y Y5 receptor.
Tsukuba Research Institute
Red-fluorescent argininamide-type NPY Y1 receptor antagonists as pharmacological tools.
Universit£T Regensburg
Discovery and evaluation of pyrazolo[1,5-a]pyrimidines as neuropeptide Y1 receptor antagonists.
Pfizer
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
N(G)-Acyl-argininamides as NPY Y(1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity.
UniversitäT Regensburg
Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists.
Glaxosmithkline
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists.
Schering-Plough Research Institute
[Lys(DOTA)4]BVD15, a novel and potent neuropeptide Y analog designed for Y1 receptor-targeted breast tumor imaging.
University of Sherbrooke
Identification of positron emission tomography ligands for NPY Y5 receptors in the brain.
Tsukuba Research Institute
Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors.
Tsukuba Research Institute
Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists.
Tsukuba Research Institute
Optimization of a series of 2,4-diaminopyridines as neuropeptide Y Y1 receptor antagonists with reduced hERG activity.
Tsukuba Research Institute
The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists.
Glaxosmithkline
8-amino-6-(arylsulphonyl)-5-nitroquinolines: novel nonpeptide neuropeptide Y1 receptor antagonists
TBA
Aryl urea derivatives of spiropiperidines as NPY Y5 receptor antagonists.
Tsukuba Research Institute
Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect.
Tsukuba Research Institute
Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist.
University of Regensburg
Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists.
UniversitäT Regensburg
Syntheses and structure-activity relationships of novel, potent, and selective trans-2-[3-oxospiro[isobenzofuran-1(3H),1'-cyclohexan]-4'-yl]benzimidazole NPY Y5 receptor antagonists.
Banyu Tsukuba Research Institute
Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4'-piperidin]-1'-yl}benzimidazole derivatives.
Banyu Tsukuba Research Institute
(9S)-9-(2-hydroxy-4,4-dimethyl-6-oxo-1-cyclohexen-1-yl)-3,3-dimethyl-2,3,4,9-tetrahydro-1H-xanthen-1-one, a selective and orally active neuropeptide Y Y5 receptor antagonist.
Tsukuba Research Institute
Novel selective neuropeptide Y2 receptor PEGylated peptide agonists reduce food intake and body weight in mice.
Bayer Pharmaceuticals
Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y
Leipzig University
A long-acting selective neuropeptide Y2 receptor PEGylated peptide agonist reduces food intake in mice.
Bayer Pharmaceuticals
Double Methotrexate-Modified Neuropeptide Y Analogues Express Increased Toxicity and Overcome Drug Resistance in Breast Cancer Cells.
Universitat Leipzig
Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar affinity.
University of Cincinnati
Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide Y Y
University of Regensburg
Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists.
Novartis Pharma
Synthesis and evaluation of substituted 4-alkoxy-2-aminopyridines as novel neuropeptide Y1 receptor antagonists.
Tsukuba Research Institute
Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y(5) antagonists.
Universidad De Navarra
Design and Evaluation of Peptide Dual-Agonists of GLP-1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis.
Syracuse University
Discovery of potent and selective small molecule NPY Y5 receptor antagonists.
Lundbeck Research Usa
Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 3: 7-methoxy-1-hydroxy-1-substituted tetraline derivatives.
Fujisawa Pharmaceutical
Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives.
Fujisawa Pharmaceutical
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
Pharmaceutical Research Institute
Novel dihydropyrazine analogues as NPY antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Engineering of a Potent, Long-Acting NPY2R Agonist for Combination with a GLP-1R Agonist as a Multi-Hormonal Treatment for Obesity.
The Scripps Research Institute
Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists.
Amgen
Highly selective and potent neuropeptide Y (NPY) Y1 receptor antagonists based on [Pro(30), Tyr(32), Leu(34)]NPY(28-36)-NH2 (BW1911U90).
University of Cincinnati and Va Medical Centers
High Affinity Agonists of the Neuropeptide Y (NPY) Y4 Receptor Derived from the C-Terminal Pentapeptide of Human Pancreatic Polypeptide (hPP): Synthesis, Stereochemical Discrimination, and Radiolabeling.
University of Regensburg
Structure-activity studies including a Psi(CH(2)-NH) scan of peptide YY (PYY) active site, PYY(22-36), for interaction with rat intestinal PYY receptors: development of analogues with potent in vivo activity in the intestine.
University of Cincinnati Medical Center
Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226.
University of Regensburg
Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists.
Novartis Pharma
Optically Pure, Structural, and Fluorescent Analogues of a Dimeric Y4 Receptor Agonist Derived by an Olefin Metathesis Approach.
Monash University (Parkville Campus)
Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R.
Monash University (Parkville Campus)
1,3-Disubstituted benzazepines as novel, potent, selective neuropeptide Y Y1 receptor antagonists.
Shionogi
Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists.
Agouron Pharmaceuticals
Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists.
Eli Lilly
Structure-activity relationships of a series of benzothiophene-derived NPY Y1 antagonists: optimization of the C-2 side chain.
Eli Lilly
Pharmacological treatment of obesity: therapeutic strategies.
The R. W. Johnson Pharmaceutical Research Institute
Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists.
Eli Lilly
Synthesis and evaluation of a series of novel 2-[(4-chlorophenoxy)methyl]benzimidazoles as selective neuropeptide Y Y1 receptor antagonists.
Eli Lilly
Bis(31/31') ([CYS(31), Trp(32), Nva(34)] NPY-(31-36)): a specific NPY Y-1 receptor antagonist.
University of Cincinnati Medical Center
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
Cnrs/Ipbs (Institut De Pharmacologie Et Biologie Structurale)
Defining structural requirements for neuropeptide Y receptors using truncated and conformationally restricted analogues.
Salk Institute
Neuropeptide Y: Y1 and Y2 affinities of the complete series of analogues with single D-residue substitutions.
Salk Institute
Recent advances in urea- and thiourea-containing compounds: focus on innovative approaches in medicinal chemistry and organic synthesis.
University of Perugia Via Del Liceo
Highly potent antiobesity effect of a short-length peptide YY analog in mice.
Takeda Pharmaceutical
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.
Pfizer
Novel cambinol analogs as sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity.
University of St. Andrews
Carbonic anhydrase inhibitors: the membrane-associated isoform XV is highly inhibited by inorganic anions.
Universita Degli Studi Di Firenze
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.
Pfizer
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
Amgen
Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development.
Gsk
[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
Abbott Laboratories
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Abbott Laboratories