Antimalarial cyclic peroxy ketals

被引：60

作者：

Posner, GH

O'Dowd, H

Ploypradith, P

Cumming, JN

Xie, S

Shapiro, TA

机构：

[1] Johns Hopkins Univ, Dept Chem, Baltimore, MD 21218 USA

[2] Johns Hopkins Univ, Sch Med, Dept Med, Baltimore, MD 21205 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1998年 / 41卷 / 12期

关键词：

D O I：

10.1021/jm980088f

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Over 20 new, cyclic, peroxy ketals have been prepared via a two-step protocol starting with readily available aryl methyl ketones. Structure-activity correlations using in vitro antimalarial data as a guide for optimization of potency have led to the design and synthesis of seven new peroxides that have IC50 values of 31-85 nM (artemisinin IC50 = 8.4 nM). Some SAR generalizations are discussed.

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收藏

页码：2164 / 2167

页数：4

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