Syntheses and antimalarial activities of 10-substituted deoxoartemisinins

被引：42

作者：

Ma, JY

Katz, E

Kyle, DE

Ziffer, H

机构：

[1] NIDDK, Phys Chem Lab, NIH, Bethesda, MD 20892 USA

[2] NIDDK, Bioorgan Chem Lab, Bethesda, MD 20892 USA

[3] Walter Reed Army Med Ctr, Walter Reed Army Inst Res, Dept Parasitol, Washington, DC 20307 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2000年 / 43卷 / 22期

关键词：

D O I：

10.1021/jm000195l

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of 10-substituted deoxoartemisinin derivatives have been synthesized. The first employed the reaction of dihydroartemisinin acetate with several silyl enol ethers in the presence of titanium tetrachloride. The second utilized the reaction of 10-(2-oxoethyl)deoxoartemisinin with several Grignard reagents. The in vitro antimalarial activities of both series were determined against two drug-resistant clones of P. falciparum. The activities of 13 beta and 15 beta were 5-7 times greater than that of artemisinin.

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页码：4228 / 4232

页数：5

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