Orally active antimalarials: Synthesis and bioevaluation of a new series of steroid-based 1.2.4-trioxanes against multi-drug resistant malaria in mice

被引：20

作者：

Singh, Chandan ^{[1
]}

Sharma, Upasana

Saxena, Gunjan

Puri, Sunil. K.

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 | 2007年 / 17卷 / 15期

关键词：

malaria; artemisinin; 1,2,4-trioxanes; steroid-based;

D O I：

10.1016/j.bmcl.2007.05.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of steroid-based 1,2,4-trioxanes 7a-f, 8a-f and 9b-e have been synthesized and evaluated for their antimalarial activity against multi-drug resistant Plasmodium yoelii in Swiss mice by oral route. The biological activity shows a strong dependence on the size and the nature of the steroidal side chain. Pregnane-based trioxanes 8a-f show better activity profile than trioxanes 7a-f and 9b-e, derived from cholesterol and tigogenine, respectively. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4097 / 4101

页数：5

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