SYNTHESIS AND ANTIMALARIAL ACTIVITY OF (+)-DEOXOARTEMISININ

被引：115

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 05期

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

页码：1516 / 1518

页数：3

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