Discovery of nonpeptide potent conformationally restricted angiotensin II receptor antagonists

A series of potent, selective, conformationally restricted angiotensin II (AII) receptor antagonists has been discovered. Two classes of conformationally restricted analogues were prepared: triazolone-based and imidazole-based biphenyl derivatives. The most active compound, an imidazole-based analog...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1994-11, Vol.4 (21), p.2591-2596
Main Authors: Huang, Horng-Chih, Chamberlain, Timothy S., Olins, Gillian M., Corpus, Valerie M., Chen, Susan T., McMahon, Ellen G., Palomo, Maria A., Blaine, Edward H., Manning, Robert E.
Format: Article
Language:English
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A series of potent, selective, conformationally restricted angiotensin II (AII) receptor antagonists has been discovered. Two classes of conformationally restricted analogues were prepared: triazolone-based and imidazole-based biphenyl derivatives. The most active compound, an imidazole-based analogue, has an IC 50 of 11 nM and a pA 2 of 8.8. A series of potent, selective, conformationally restricted angiotensin II (AII) receptor antagonists has been discoveed. The most active compound, an imidazole-based analogues, has an IC 50 of 11 nM and a pA 2 of 8.8.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80290-0