SYNTHESIS AND ANTIMALARIAL ACTIVITY OF (+)-DEOXOARTEMISININ

被引:114
|
作者
JUNG, M [1 ]
LI, X [1 ]
BUSTOS, DA [1 ]
ELSOHLY, HN [1 ]
MCCHESNEY, JD [1 ]
MILHOUS, WK [1 ]
机构
[1] WALTER REED ARMY MED CTR,DIV EXPTL THERAPEUT,WASHINGTON,DC 20307
关键词
D O I
10.1021/jm00167a036
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
(+)-Deoxoartemisinin (2), a new and more active antimalarial agent, was successfully prepared from artemisinin in one step using NaBH4 and BF3-Et2O in THF. (-)-Deoxodeoxyartemisinin (5), a potential metabolite of deoxo- artemisinin, was also prepared either from 2 or from artemisinic acid. 2 shows 8-fold increased antimalarial activity in vitro against chloroquine-resistant malaria as compared to artemisinin (1). Compound 2 possesses superior in vivo antimalarial activity to 1. © 1990, American Chemical Society. All rights reserved.
引用
收藏
页码:1516 / 1518
页数:3
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