AGENTS FOR THE TREATMENT OF OVERACTIVE DETRUSOR .1. SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF 1,1'-BIPHENYL DERIVATIVES

被引：0
|
作者：
TAKE, K [1 ]
OKUMURA, K [1 ]
TAKIMOTO, K [1 ]
KATO, M [1 ]
OHTSUKA, M [1 ]
SHIOKAWA, Y [1 ]
机构：
[1] FUJISAWA PHARMACEUT CO LTD, PROD DEV LABS, OSAKA 532, JAPAN
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1991年 / 39卷 / 11期
关键词：
OVERACTIVE DETRUSOR; INHIBITORY ACTIVITY; ELECTRICAL FIELD STIMULATION; 1,1'-BIPHENYL-2,6-DICARBOXYLIC ACID DIESTER;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 1,1'-biphenyl-2,6-dicarboxylic acid diesters were synthesized and examined for their inhibitory activity on guinea-pig detrusor muscle contraction at electrical field stimulation in vitro. Among them, 6-isopropyl 2-methyl 3-hydroxy-5-methyl-2'-nitro-(1,1'-biphenyl)-2,6-dicarboxylate, FR75513 (8a) was one of the potent compounds (IC50 = 3.3 x 10(-6) g/ml). This compound (8a) exhibited a strong inhibitory activity on detrusor contraction after intravenous administration in anesthetized rats (ID50 = 0.04 mg/kg).
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页码：2915 / 2923
页数：9
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