SYNTHESIS OF HALOGEN-SUBSTITUTED 1,5-BENZOTHIAZEPINE DERIVATIVES AND THEIR VASODILATING AND HYPOTENSIVE ACTIVITIES

被引：82

作者：

INOUE, H ^{[1
]}

KONDA, M ^{[1
]}

HASHIYAMA, T ^{[1
]}

OTSUKA, H ^{[1
]}

TAKAHASHI, K ^{[1
]}

GAINO, M ^{[1
]}

DATE, T ^{[1
]}

AOE, K ^{[1
]}

TAKEDA, M ^{[1
]}

MURATA, S ^{[1
]}

NARITA, H ^{[1
]}

NAGAO, T ^{[1
]}

机构：

[1] TANABE SEIYAKU CO LTD,BIOL RES LAB,TODA,SAITAMA 335,JAPAN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 02期

关键词：

D O I：

10.1021/jm00106a032

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In an attempt to improve the effectiveness and duration of the action of diltiazem (1), a 1,5-benzothiazepine calcium channel blocker, its derivatives (2) with halogen substituents on the fused benzene ring were synthesized. These compounds were evaluated for their effects on vertebral and coronary blood flows and antihypertensive activity. The structure-activity relationships are discussed. The 8-chloro derivative ((+)-2b), the most potent compound in this series, was selected for clinical evaluation as a cerebral vasodilating and antihypertensive agent.

引用

页码：675 / 687

页数：13

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