A NEW CLASS OF ANGIOTENSIN-II RECEPTOR ANTAGONISTS WITH A NOVEL ACIDIC BIOISOSTERE

Authors
KOHARA Y IMAMIYA E KUBO K WADA T INADA Y NAKA T
Citation
Y. Kohara et al., A NEW CLASS OF ANGIOTENSIN-II RECEPTOR ANTAGONISTS WITH A NOVEL ACIDIC BIOISOSTERE, Bioorganic & medicinal chemistry letters, 5(17), 1995, pp. 1903-1908
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
17
Year of publication
1995
Pages
1903 - 1908
Database
ISI
SICI code
0960-894X(1995)5:17<1903:ANCOAR>2.0.ZU;2-4
Abstract
The synthesis and angiotensin II (AII) antagonistic activity of 2-subs tituted benzimidazole-7-carboxylic acids (8) bearing a novel acidic bi oisostere, a 5-oxo-1,2,4-oxadiazole ring, are described. These compoun ds had in vitro and in vivo AII receptor antagonistic activity compara ble to that of tetrazole analogs. The representative compound, TAK-536 (8 e) is a potent, orally active and specific AII receptor antagonist .