Orally active amino functionalized antimalarial 1,2,4-trioxanes

被引：63
作者：
Singh, C [1 ]
Malik, H
Puri, SK
机构：
[1] Cent Drug Res Inst, Div Med Chem, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 02期
关键词：
D O I：
10.1016/j.bmcl.2003.10.051
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Using readily available trioxanes 6a-b, a new series of amino functionalized 1,2,4-trioxanes 8a-e and 9a-e have been prepared and evaluated for antimalarial activity against multi-drug resistant Plasmodium yoelii in Swiss mice model. Several of these novel trioxanes are orally more active than the parent trioxanes 6a-b. Antimalarial activity of amino functionalized trioxane 9a, the most potent compound in the series, is very close to that of beta-arteether. (C) 2003 Elsevier Ltd. All rights reserved.
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页码：459 / 462
页数：4
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