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
收藏
页码：5190 / 5193
页数：4
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