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

被引:8
作者
ALLOTT, CP
BRADBURY, RH
DENNIS, M
FISHER, E
LUKE, RWA
MAJOR, JS
OLDHAM, AA
PEARCE, RJ
REID, AC
ROBERTS, DA
RUDGE, DA
RUSSELL, ST
机构
[1] Departments of Chemistry and Bioscience, ICI Pharmaceuticals, Mereside, Macclesfield, Cheshire SK10 4TG, Alderley Park
关键词
D O I
10.1016/S0960-894X(00)80689-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Quinoline-, 1,5-naphthyridine- and pyridine-based angiotensin II antagonists are reported. The more potent compounds gave IC50 values of ca 0.01 muM in a guinea pig adrenal membrane binding assay and intravenous ED50 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.
引用
收藏
页码:899 / 904
页数:6
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