DISCOVERY OF NONPEPTIDE, POTENT CONFORMATIONALLY RESTRICTED ANGIOTENSIN-II RECEPTOR ANTAGONISTS

Authors
HUANG HC CHAMBERLAIN TS OLINS GM CORPUS VM CHEN ST MCMAHON EG PALOMO MA BLAINE EH MANNING RE
Citation
Hc. Huang et al., DISCOVERY OF NONPEPTIDE, POTENT CONFORMATIONALLY RESTRICTED ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(21), 1994, pp. 2591-2596
Citations number
25
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
21
Year of publication
1994
Pages
2591 - 2596
Database
ISI
SICI code
0960-894X(1994)4:21<2591:DONPCR>2.0.ZU;2-E
Abstract
A series of potent, selective, conformationally restricted angiotensin II (AII) receptor antagonists has been discovered Two classes of conf ormationally restricted analogues were prepared: triazolone-based and imidazole-based biphenyl derivatives. The mast active compound, an imi dazole-based analogue, has an IC50 of 11 nM and a pA(2) of 8.8.