PARTIAL SYNTHESIS OF 6'-HYDROXYCINCHONINE AND ITS ANTI-ARRHYTHMIC ACTIVITY IN MICE

被引:19
作者
SMALL, LD
ROSENBERG, H
NWANGWU, PU
HOLCSLAW, TL
STOHS, SJ
机构
[1] College of Pharmacy, University of Nebraska Medical Center, Omaha
关键词
D O I
10.1021/jm00194a027
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of 6ʹ-hydroxycinchonine [(8fl, 9S)-cinchonan-6ʹ, 9-diol] was achieved by demethylating quinidine with boron tribromide in dichloromethane at -75°C. The antiarrhythmic activities of 6ʹ-hydroxycinchonine and quinidine were compared following the infusion of aconitine into the tail veins of mice to induce arrhythmias. Comparative ED50 and LD50 studies for quinidine and 6ʹ-hydroxycinchonine revealed equivalent antiarrhythmic potencies for the two drugs but a smaller acute toxicity for 6ʹ-hydroxycinchonine. © 1979, American Chemical Society. All rights reserved.
引用
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页码:1014 / 1016
页数:3
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