A CONFORMATIONALLY RESTRAINED SERIES OF AT(1)-SELECTIVE ANGIOTENSIN-II ANTAGONISTS

被引:7
作者
CARPINO, PA
SNEDDON, SF
JARDINE, PD
MAGNUSAYRITEY, GT
RAUCH, AL
BURKARD, MR
机构
[1] PFIZER INC,CENT RES,DEPT COMP CHEM,GROTON,CT 06340
[2] PFIZER INC,CENT RES,DEPT METAB DIS,GROTON,CT 06340
关键词
D O I
10.1016/S0960-894X(01)81128-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The benzyl linker in the angiotensin II receptor antagonist L-158,809 that separates the imidazo[4,5-b]pyridine ring and the 2-tetrazolylphenyl group was replaced by a series of bicyclic rings. The optimal bicyclic ring was found to be a dihydroindanyl group. Modification of the imidazo[4,5-b]pyridine group resulted in the discovery of a rigid analog that was as potent as L-158,809.
引用
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页码:93 / 98
页数:6
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