Seifert Karin, Lemke Andreas, Croft Simon L, Kayser Oliver
Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, United Kingdom.
Antimicrob Agents Chemother. 2007 Dec;51(12):4525-8. doi: 10.1128/AAC.00465-07. Epub 2007 Oct 1.
Antileishmanial activities of 91 synthetic phospholipids against Leishmania donovani were evaluated in vitro and cytotoxicity assessed against two mammalian cell lines. Promising compounds were tested further in vivo. In vitro structure-activity relationships showed a positive contribution of head groups bearing ring systems (N-methylpiperidino and N-methylmorpholino) to antileishmanial activity.
评估了91种合成磷脂对杜氏利什曼原虫的抗利什曼活性,并针对两种哺乳动物细胞系评估了细胞毒性。对有前景的化合物进行了进一步的体内试验。体外构效关系表明,带有环系统的头部基团(N-甲基哌啶基和N-甲基吗啉基)对抗利什曼活性有积极贡献。