Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University , Bornova, Izmir , Turkey.
J Enzyme Inhib Med Chem. 2013 Oct;28(5):960-7. doi: 10.3109/14756366.2012.697058. Epub 2012 Jul 18.
A series of substituted phenylethylidenehydrazinylpyridinium derivatives bearing methyl, ethyl, propyl, and propylphenyl groups on the pyridinium nitrogen were synthesized and evaluated for in vitro antileishmanial activity against Leishmania tropica by using the microdilution method. Among the tested compounds, 3d, 5c, 3b, and 3c were found to be the most active derivatives against the promastigotes of L. tropica (IC50 values are 6.90, 9.92, 11.69 and 12.03 µM, respectively) and to be more active than reference drug meglumine antimonaite (glucantime) (IC50 value: 20.49 µM). The derivatives investigated in this study may have the potential to be lead compound against leishmanial infection.
一系列取代的苯乙基亚肼基吡啶鎓衍生物，吡啶鎓氮上带有甲基、乙基、丙基和丙基苯基，通过微量稀释法评估其对利什曼原虫（Leishmania tropica）的体外抗利什曼原虫活性。在所测试的化合物中，3d、5c、3b 和 3c 对利什曼原虫的前鞭毛体表现出最强的活性（IC50 值分别为 6.90、9.92、11.69 和 12.03 μM），并且比参考药物葡甲胺锑（glucantime）（IC50 值：20.49 μM）更具活性。本研究中研究的衍生物可能具有成为抗利什曼原虫感染的潜在先导化合物的潜力。
