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Quinoxaline N-oxide containing potent angiotensin II receptor antagonists: synthesis, biological properties, and structure-activity relationships.

Bristol-Myers Squibb Pharmaceutical Research Institute

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

Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype.

Warner-Lambert

 

4,5-Dihydro-4-oxo-3H-imidazo[4,5-c]pyridines: potent arylacetic acid-derived AT₁ antagonists with improved affinity for the AT₂ receptor

TBA

 

Balanced AT₁ and AT₂ angiotensin II antagonists. II. Potent 5 α-hydroxyacid imidazolyl biphenyl sulfonylureas

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

 

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. I. The effects of biphenyl “ortho”-substitution on AT₁/AT₂ affinities

TBA

Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Multiple binding modes for the receptor-bound conformations of cyclic AII agonists.

Washington University

A novel series of selective, non-peptide inhibitors of angiotensin II binding to the AT2 site.

Dupont Pharmaceuticals

Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification.

University of Innsbruck

Bicyclic tripeptide mimetics with reverse turn inducing properties.

Uppsala University

Angiotensin II analogues encompassing 5,9- and 5,10-fused thiazabicycloalkane tripeptide mimetics.

Uppsala University

Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.

Wyeth-Ayerst Research

Design, synthesis, and biological activities of four angiotensin II receptor ligands with gamma-turn mimetics replacing amino acid residues 3-5.

Uppsala University

4-Diazinyl- and 4-pyridinylimidazoles: potent angiotensin II antagonists. A study of their activity and computational characterization.

Laboratori Guidotti

Sulfonylureas and sulfonylcarbamates as new non-tetrazole angiotensin II receptor antagonists. Discovery of a highly potent orally active (imidazolylbiphenylyl)sulfonylurea (HR 720).

Hoechst Roussel Pgu Cardiovascular Agents

Pyrido[2,3-d]pyrimidine angiotensin II antagonists.

Wyeth-Ayerst Research

Conformational restriction of angiotensin II: cyclic analogues having high potency.

G.D. Searle And