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).

引用

页码：2915 / 2923

页数：9

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