Synthesis and in vitro activities of ferrocenic aminohydroxynaphthoquinones against Toxoplasma gondii and Plasmodium falciparum

被引：117

作者：

Baramee, A

Coppin, A

Mortuaire, M

Pelinski, L ^{[1
]}

Tomavo, S

Brocard, J

机构：

[1] USTL, ENSCL, CNRS,Grp Synth Asymetr & Mol Therapeut, UMR 8010,Lab Catalyse Lille, F-59652 Villeneuve Dascq, France

[2] Chiang Mai Univ, Fac Sci, Dept Chem, Chiang Mai 50200, Thailand

[3] USTL, CNRS, UMR 8576, Equipe Parasitol Mol,Unit Glycobiol Struct & Fonc, F-59650 Villeneuve Dascq, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 05期

关键词：

anti-malarial activity; atovaquone; ferrocene; toxoplasmosis;

D O I：

10.1016/j.bmc.2005.09.054

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Fourteen ferrocenyl aminohydroxynaphthoquinones, analogues of atovaquone, were synthesized from the hydroxynaphthoquinone core. These novel atovaquone derivatives were tested for their in vitro activity against two apicomplexan parasites of medical importance, Toxoplasma gondii and Plasmodium falciparum, including resistant strains to atovaquone (T gondii) and chloroquine (P. falciparum). Three of these ferrocenic atovaquone derivatives composed of the hydroxynaphthoquinone core plus an amino-ferrocenic group and an aliphatic chain with 6-8 carbon atoms were found to be significantly active against T gondii. Moreover, these novel compounds were also effective against the atovaquone-resistant strain of T. gondii (Ato(R)). (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1294 / 1302

页数：9

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