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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, 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

Tactical Approaches to Interconverting GPCR Agonists and Antagonists.

University of Minnesota

Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.

Uppsala University

Imidazopyridines as a source of biological activity and their pharmacological potentials-Infrared and Raman spectroscopic evidence of their content in pharmaceuticals and plant materials.

Wroclaw University of Economics

Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands.

Uppsala University

Saralasin and Sarile Are AT2 Receptor Agonists.

Universit£

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

Bristol-Myers Squibb Pharmaceutical Research and Development

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

Synthesis of a new class of druglike angiotensin II C-terminal mimics with affinity for the AT2 receptor.

Uppsala University

Design, synthesis, and incorporation of a beta-turn mimetic in angiotensin II forming novel pseudopeptides with affinity for AT1 and AT2 receptors.

Uppsala University

Angiotensin II pseudopeptides containing 1,3,5-trisubstituted benzene scaffolds with high AT2 receptor affinity.

Uppsala University

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

New selective AT2 receptor ligands encompassing a gamma-turn mimetic replacing the amino acid residues 4-5 of angiotensin II act as agonists.

Uppsala University

AT2-selective angiotensin II analogues containing tyrosine-functionalized 5,5-bicyclic thiazabicycloalkane dipeptide mimetics.

Uppsala University

Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.

Uppsala University

New analgesic drugs derived from phencyclidine.

TBA

A selective AT2 receptor ligand with a gamma-turn-like mimetic replacing the amino acid residues 4-5 of angiotensin II.

Uppsala University

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

 

L-161,638: A potent AT2selective quinazolinone angiotensin II binding inhibitor

TBA

 

1,4-substituted indoles: a potent and selective class of angiostensin II receptor antagonists

TBA

 

The syntheses and binding affinities of tools for the study of angiotensin AT2 receptors

TBA

Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazole derivatives as nonpeptidic angiotensin II AT1 receptor antagonists.

Beijing Institute of Technology

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

 

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

 

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

 

AT₁ selective angiotensin II antagonists with phenoxyphenylacetic acid as a biphenyl replacement part I

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

 

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

 

Balanced angiotensin II receptor antagonists. I. The effects of biphenyl “ortho”-substitution on AT₁/AT₂ affinities

TBA

 

Imidazolinones as nonpeptide 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

 

Tetrahydroisoquinoline derivatives with AT₂-specific angiotensin II reception binding inhibitory activity

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

 

Imidazo[4,5-b]pyridine-based AT₁ / AT₂ angiotensin II receptor antagonists

TBA

 

Triazolinones as nonpeptide angiotensin II antagonists. 2. discovery of a potent and orally active triazolinone acylsulfonamide

TBA

 

Angiotensin II receptor antagonists containing a phenylpyridine element.

TBA

 

4,5,6,7-Tetrahdryo-8-oxo-cycloheptimidazoles: a new class of potent non-peptide angiiotensin II receptor antagonists

TBA

 

Synthesis and structure-activity relationships of a novel series of non-peptide AT₂-selective angiotensin II receptor antagonists

TBA

Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.

Merck Research Laboratories

Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships.

Uppsala University

First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo.

Uppsala University

The Other Angiotensin II Receptor: AT

Centre Hospitalier Universitaire Vaudois (Chuv) and University of Lausanne (Unil

Discovery of TD-0212, an Orally Active Dual Pharmacology AT

Theravance Biopharma Us

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

Washington University

Nonpeptide angiotensin II antagonists: N-phenyl-1H-pyrrole derivatives are angiotensin II receptor antagonists.

Searle

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

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

Dupont Pharmaceuticals

(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.

Merck Research Laboratories

A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor.

Merck Research Laboratories

Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.

E. Merck

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 AT? receptor antagonists derived from 6-substituted aminocarbonyl and acylamino benzimidazoles.

Beijing Institute of Technology

Synthesis and SAR studies of novel triazolopyrimidine derivatives as potent, orally active angiotensin II receptor antagonists.

Carpibem

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

Balanced AT1/AT2 receptor antagonists. 4. XR510 and related 5-(3-amidopropanoyl)imidazoles possessing equal affinity for the AT1 and AT2 receptors.

Dupont Pharmaceuticals

Derivatives of 5-[[1-(4'-carboxybenzyl)imidazolyl]methylidene]hydantoins as orally active angiotensin II receptor antagonists.

Warner-Lambert

Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes.

Merck Research Laboratories

Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.

Universitaire Vaudois

1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists.

Smithkline Beecham Pharmaceuticals

SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.

Sanofi-Synthelabo Recherche

N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.

Pudue Pharma Discovery Research

Binding of KRH-594, an antagonist of the angiotensin II type 1 receptor, to cloned human and rat angiotensin II receptors.

Shinshu University

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.

Abbott Laboratories

Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.

SynthÉLabo Recherche

Pharmacologic characterization of CI-996, a new angiotensin receptor antagonist.

Parke-Davis Pharmaceutical Research

In vivo receptor occupancy of the angiotensin II receptor by nonpeptide antagonists: relationship to in vitro affinities and in vivo pharmacologic potency.

Merck Research Laboratories

Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, U-97018.

Upjohn Pharmaceuticals

(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.

Abbott Laboratories