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Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoroacetyl)-1H-pyrrol-1-yl]-1H- imidazole-5-car

Warner-Lambert

New nonpeptide angiotensin II receptor antagonists. 1. Synthesis, biological properties, and structure-activity relationships of 2-alkyl benzimidazole derivatives.

Ici Pharmaceuticals Group

Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.

Exploratory Chemistry Merck Sharp And Dohme Research Laboratories

Synthesis and biological activity of angiotensin II analogues containing a Val-His replacement, Val psi[CH(CONH2)NH]His.

Berlex Laboratories

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

Saralasin and Sarile Are AT2 Receptor Agonists.

Universit£

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

The replacement of His(4) in angiotensin IV by conformationally constrained residues provides highly potent and selective analogues.

Vrije Universiteit Brussel

Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research And Development

Chemokine receptor antagonists.

National Heart And Lung Institute

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

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.

Technische Universit£T Darmstadt

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

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 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

 

D and L-N-[(1-benzyl-1H-imidazol-5-yl)-alkyl]-amino acids as angiotensin II AT-1 antagonists

TBA

 

Potent triazolinone-based angiotensin II receptor antagonists with equivalent affinity for both the AT₁ and AT₂ subtypes

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

 

Imidazolinones as nonpeptide angiotensin II receptor antagonists

TBA

 

Valsartan, a potent, orally active angiotensin II antagonist developed from the structurally new amino acid series

TBA

 

A potent long-acting imidazole-5-acrylic acid angiotensin II AT-1 receptor antagonist

TBA

Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.

Pfizer

An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.

Predix Pharmaceuticals

Recognition of privileged structures by G-protein coupled receptors.

Novo Nordisk

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

Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT(1) angiotensin II receptor antagonists.

Université

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

High accuracy in silico sulfotransferase models.

Albert Einstein College Of Medicine

Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.

Yogi Vemana University

Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.

University Of Leipzig

1,3-disubstituted-4-aminopyrazolo [3, 4-d] pyrimidines, a new class of potent inhibitors for phospholipase D.

University Of Massachusetts Boston