Quinoline, 1,5-naphthyridine and pyridine derivatives as potent, nonpeptidic angiotensin II receptor antagonists

Abstract Quinoline-, 1,5-naphthyridine- and pyridine-based angiotensin II antagonists are reported. The more potent compounds gave IC 50 values of ca 0.01 μM in a guinea pig adrenal membrane binding assay and intravenous ED 50 values in the range 0.1–1.0 mg/kg for inhibition of the AII-induced pressor response in normotensive rats. Several of these compounds, for example 4d (ICI D6888), showed good oral activity in this animal model.