QUINOLINE, 1,5-NAPHTHYRIDINE AND PYRIDINE-DERIVATIVES AS POTENT, NONPEPTIDIC ANGIOTENSIN-II RECEPTOR ANTAGONISTS

Authors
ALLOTT CP BRADBURY RH DENNIS M FISHER E LUKE RWA MAJOR JS OLDHAM AA PEARCE RJ REID AC ROBERTS DA RUDGE DA RUSSELL ST
Citation
Cp. Allott et al., QUINOLINE, 1,5-NAPHTHYRIDINE AND PYRIDINE-DERIVATIVES AS POTENT, NONPEPTIDIC ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 3(5), 1993, pp. 899-904
Citations number
51
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
5
Year of publication
1993
Pages
899 - 904
Database
ISI
SICI code
0960-894X(1993)3:5<899:Q1APAP>2.0.ZU;2-G
Abstract
Quinoline-, 1,5-naphthyridine- and pyridine-based angiotensin II antag onists are reported. The more potent compounds gave IC50 values of ca 0.01 muM in a guinea pig adrenal membrane binding assay and intravenou s ED50 values in the range 0.1-1.0 mg/kg for inhibition of the AII-ind uced pressor response in normotensive rats. Several of these compounds , for example 4d (ICI D6888), showed good oral activity in this animal model.