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

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
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.