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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

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

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

 

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

 

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

 

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

 

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

TBA

 

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

Squaric acid analogues in medicinal chemistry.

Palacky University Olomouc

2-Alkyl substituted benzimidazoles as a new class of selective AT2 receptor ligands.

Uppsala University

Angiotensin II AT2 receptor ligands with phenylthiazole scaffolds.

Uppsala University

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

Uppsala University

Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability.

Vrije Universiteit Brussel

N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.

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

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

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

Beijing Institute of Technology

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

SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.

Smithkline Beecham Pharmaceuticals

Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.

Kudos Pharmaceuticals

Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.

Boehringer Ingelheim (Canada)

Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity.

Uppsala University

Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.

University of Newcastle