Probing the role of the covalent linkage of ferrocene into a chloroquine template

被引：89

作者：

Biot, Christophe

Daher, Wassim

Ndiaye, Cheikh M.

Melnyk, Patricia

Pradines, Bruno

Chavain, Natascha

Pellet, Alain

Fraisse, Laurent

Pelinski, Lydie

Jarry, Christian

Brocard, Jacques

Khalife, Jamal

Forfar-Bares, Isabelle

Dive, Daniel

机构：

[1] USTL, ENSCL, UMR CNRS 8181, Unite Catalyse & Chim Solide, F-59652 Villeneuve Dascq, France

[2] Inst Pasteur, Inserm U547, F-59019 Lille, France

[3] Univ Lille 1, UMR CNRS 8161, F-59019 Lille, France

[4] Univ Lille 2, UMR CNRS 8161, IPL, F-59019 Lille, France

[5] Inst Trop Med, Serv Sante Armees, Unite Parasitol, F-13998 Marseille, France

[6] Sanofi Aventis Rech, Discovery Dept, F-31000 Toulouse, France

[7] Univ Bordeaux 2, F-33076 Bordeaux, France

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 15期

关键词：

D O I：

10.1021/jm060259d

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A new therapeutic approach to malaria led to the discovery of ferroquine (FQ, SR97276). To assess the importance of the linkage of the ferrocenyl group to a 4-aminoquinoline scaffold, two series of 4-aminoquinolines, structurally related to FQ, were synthesized. Evaluation of antimalarial activity, physicochemical parameters, and the beta-hematin inhibition property indicate that the ferrocene moiety has to be covalently flanked by a 4-aminoquinoline and an alkylamine. Current data reinforced our choice of FQ as a drug candidate.

引用

页码：4707 / 4714

页数：8

共 21 条

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