Synthesis and antimalarial activity of new atovaquone derivatives

被引：25

作者：

El Hage, Salome ^{[1
]}

Ane, Michele ^{[1
]}

Stigliani, Jean-Luc ^{[1
]}

Marjorie, Maynadier ^{[2
]}

Vial, Henri ^{[2
]}

Baziard-Mouysset, Genevieve ^{[1
]}

Payard, Marc ^{[1
]}

机构：

[1] Univ Toulouse 3, Fac Pharm, Lab Chim Pharmaceut, F-31062 Toulouse 09, France

[2] Dept Biol Sante, UMR 5539, F-34095 Montpellier 5, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 11期

关键词：

Plasmodium falciparum; Atovaquone; Antimalarial activity; HYDROXYNAPHTHOQUINONE; INHIBITORS;

D O I：

10.1016/j.ejmech.2009.07.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this paper we describe the design and synthesis of 18 derivatives of the antimicrobial atovaquone which were substituted at the 3-hydroxy group by ester and ether functions. The compounds were evaluated in vitro for their activity against the growth of Plasmodium falciparum, the malaria causing parasite. All the compounds showed potent activity, with IC50 values in the range of 1.25-50 nM, comparable to those of atovaquone and much higher than chloroquine or quinine. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：4778 / 4782

页数：5

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