NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - N-[(BENZYLOXY)BENZYL]IMIDAZOLES AND RELATED-COMPOUNDS AS POTENT ANTIHYPERTENSIVES

被引:97
作者
CARINI, DJ [1 ]
DUNCIA, JV [1 ]
JOHNSON, AL [1 ]
CHIU, AT [1 ]
PRICE, WA [1 ]
WONG, PC [1 ]
TIMMERMANS, PBMW [1 ]
机构
[1] DUPONT CO INC,DEPT MED PROD,CARDIOVASC PHARMACOL SECT,EXPTL STN,WILMINGTON,DE 19880
关键词
D O I
10.1021/jm00167a008
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of compounds has been synthesized and demonstrated to be antagonists of the angiotensin II (All) receptor. These compounds are structurally related to the N-(benzamidobenzyl)imidazoles and extend the scope of this new class of nonpeptide All antagonists. It has been found that the amide linkage (X = NHCO) in the N-(benzamidobenzyl)imidazoles can be replaced successfully by a variety of groups (X = single bond, O, S, CO, OCH2, CH=CH, NHCONH); linkers of 0-1 atoms in length are most effective. When administered intravenously to awake renal hypertensive rats, these compounds are potent antihypertensives. © 1990, American Chemical Society. All rights reserved.
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收藏
页码:1330 / 1336
页数:7
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