Departamento de Parasitologia, Microbiologia e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Juiz de Fora, M.G. 36036-900, Brasil.
Chem Biol Drug Des. 2010 Jun;75(6):628-31. doi: 10.1111/j.1747-0285.2010.00962.x. Epub 2010 Mar 12.
We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3). Hydrolysis of the methyl ester adduct (5) yielded the free acid (6). The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.
我们在此报告 4,7-二氯喹啉（1）与色胺（2）和 D-色氨酸甲酯（3）的缩合反应。甲酯加合物（5）经水解得到游离酸（6）。评估了这些化合物对四种不同种属的利什曼原虫前鞭毛体的体外活性和对 Kb 和 Vero 细胞的细胞毒性活性。化合物（5）对所测试的利什曼物种表现出良好的活性，而所有三种化合物在 Kb 和 Vero 细胞中均表现出中等活性。
