Biot Christophe, Daher Wassim, Chavain Natascha, Fandeur Thierry, Khalife Jamal, Dive Daniel, De Clercq Erik
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 May 4;49(9):2845-9. doi: 10.1021/jm0601856.
Three ferroquine (FQ) derivatives, closely mimicking the antimalarial drug hydroxychloroquine (HCQ), have been prepared. Whereas these organometallic compounds provide the expected reduced cytotoxic effects compared to FQ, they inhibit in vitro growth of Plasmodium falciparum far better than chloroquine (CQ). Moreover, this new class of bioorganometallic compounds exert antiviral effects with some selectivity toward SARS-CoV infection. These new drugs may offer an interesting alternative for Asia where SARS originated and malaria has remained endemic.
已制备出三种紧密模拟抗疟药物羟氯喹(HCQ)的铁喹(FQ)衍生物。与FQ相比,这些有机金属化合物的细胞毒性作用预期会降低,它们在体外对恶性疟原虫生长的抑制作用远优于氯喹(CQ)。此外,这类新型生物有机金属化合物对严重急性呼吸综合征冠状病毒(SARS-CoV)感染具有一定选择性地发挥抗病毒作用。这些新药可能为SARS起源且疟疾仍为地方病的亚洲提供一个有趣的替代选择。