DISCOVERY AND DEVELOPMENT OF ARYL-FUSED IMIDAZOLE-BASED ANGIOTENSIN-II ANTAGONISTS

Authors
MIYAKE K MATSUKURA M YONEDA N HIROSHIMA O MORI N ISHIHARA H MUSHA T MATSUOKA T SHOJI T MINAMI N HAMANO S SAITO I
Citation
K. Miyake et al., DISCOVERY AND DEVELOPMENT OF ARYL-FUSED IMIDAZOLE-BASED ANGIOTENSIN-II ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(1), 1994, pp. 213-218
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
1
Year of publication
1994
Pages
213 - 218
Database
ISI
SICI code
0960-894X(1994)4:1<213:DADOAI>2.0.ZU;2-O
Abstract
A phenolic benzofuran derivative 1 was identified as an angiotensin II receptor antagonist by random screening. Structural modifications led to a novel series of N-(4-hydroxyphenylmethyl)benzimidazoles and imid azo[4,5-b]pyridines, some of which inhibited angiotensin II-induced co ntractions in rabbit aortic strips with pA(2) values of nearly 9. The related biphenylmethyl derivative E4177 showed potent and long-lasting activity in vivo.