New functionalized 1,2,4-trioxepanes:: Synthesis and antimalarial activity against multi-drug resistant P. yoelii in mice

被引：7

作者：

Singh, Chandan ^{[1
]}

Pandey, Shilpi ^{[1
]}

Kushwaha, Ambuj K. ^{[2
]}

Puri, Sunil K. ^{[2
]}

机构：

[1] Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226001, Uttar Pradesh, India

[2] Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 19期

关键词：

antimalarial; artemisinin; 1,2,4-trioxane; 1,2,4-trioxepane; amino functionalized trioxepane; ester functionalized trioxepane;

D O I：

10.1016/j.bmcl.2008.08.096

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new amino functionalized 1,2,4-trioxepanes8-16 and ester functionalized 1,2,4-trioxepanes 17-19 have been synthesized and evaluated against multi-drug resistant Plasmodium yoelii in Swiss mice. Amino functionalized trioxepanes 14, the most active compound of the series, showed 100% clearance of parasitaemia by oral route on day 4 and 75% protection to the treated mice beyond day 28. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5190 / 5193

页数：4

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