SYNTHESIS AND BRADYCARDIAC ACTIVITY OF A SERIES OF SUBSTITUTED 3-AMINOALKYL-2,3-DIHYDRO-4H-1,3-BENZOXAZIN-4-ONES AS POTENT ANTIISCHEMICS

被引：5

作者：

RIEU, JP

DUFLOS, A

TRISTANI, JC

PATOISEAU, JF

TISNEVERSAILLES, J

BESSAC, AM

BONNAFOUS, R

MARTY, A

VERSCHEURE, Y

BIGG, DCH

机构：

[1] CTR RECH PIERRE FABRE,DIV CHIM MED 1,CASTRES,FRANCE

[2] CTR RECH PIERRE FABRE,DIV PHARMACOL CARDIOVASC 2,F-81106 CASTRES,FRANCE

[3] PIERRE FABRE MED DEV,CARDIOVASC PROJET,F-31319 LABEGE INNOPOLE,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 28卷 / 09期

关键词：

3-AMINOALKYL-2,3-DIHYDRO-4H-1,3-BENZOXAZINE-4-ONES; BRADYCARDIAC; ANTIARRHYTHMIC AND ANTIISCHEMIC AGENTS;

D O I：

10.1016/0223-5234(93)90027-C

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2,3-dihydro-4H-1,3-benzoxazin-4-ones substituted at the 3-position with an arylalkyaminoalkyl group have been synthesized and their specific bradycardic and antiarrythmic activities evaluated. Bradycardia is optimal when the aromatic rings are substituted with methoxy groups and the side-chain amine is N-methylated. N-Demethylated and 2-alkylated derivatives show the highest antiarrhythmic activity but have little bradycardid action. Most of the compounds described are more potent than Falipamil. Compound lm (F 3226) has been selected for further pharmacological tests and the bradycardic activity has been confirmed when administered orally to anesthetized rats without notable side effects.

引用

页码：683 / 691

页数：9