Antimalarial sulfone trioxanes

被引：42

作者：

Posner, GH ^{[1
]}

O'Dowd, H

Caferro, T

Cumming, JN

Ploypradith, P

Xie, SJ

Shapiro, TA

机构：

[1] Johns Hopkins Univ, Sch Arts & Sci, Dept Chem, Baltimore, MD 21218 USA

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

来源：

TETRAHEDRON LETTERS | 1998年 / 39卷 / 16期

关键词：

D O I：

10.1016/S0040-4039(98)00290-1

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of new sulfide and sulfone 1,2,4-trioxanes was prepared in only a few steps from commercial reactants. The sulfone trioxanes were found to have higher in vitro antimalarial potencies than the sulfides, with 12 beta-arylsulfone trioxanes 1 beta being from 1/3 to 1/4 as potent as the complex natural antimalarial trioxane artemisinin (2). A tentative chemical mechanism is proposed to account for the great difference in antimalarial activity of the 12 alpha-vs. 12 beta-sulfide trioxanes. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2273 / 2276

页数：4

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