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
Unité de Catalyse et Chimie du Solide - UMR CNRS 8181, ENSCL, Bâtiment C7, USTL, B.P. 90108, 59652, Villeneuve d' Ascq Cedex, France.
J Med Chem. 2006 Jul 27;49(15):4707-14. doi: 10.1021/jm060259d.
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.
一种针对疟疾的新治疗方法促成了铁喹啉（FQ，SR97276）的发现。为评估二茂铁基与4-氨基喹啉骨架连接的重要性，合成了与FQ结构相关的两个系列的4-氨基喹啉。抗疟活性、理化参数及β-血红素抑制特性评估表明，二茂铁部分必须由一个4-氨基喹啉和一个烷基胺共价连接。目前的数据强化了我们将FQ选为候选药物的选择。
