Molecular Virology and Infectious Diseases Section, Department of Biological and Medical Research, King Faisal Specialist Hospital and Research Centre, Riyadh, Saudi Arabia.
Saudi Pharm J. 2009 Jul;17(3):227-32. doi: 10.1016/j.jsps.2009.08.005. Epub 2009 Aug 7.
Leishmania donovani, the causative agent of visceral leishmaniasis, is transmitted by sand flies and replicates intracellularly in their mammalian host cells. The emergence of drug-resistant strains has hampered efforts to control the spread of the disease worldwide. Forty-four 1,3,4-thiadiazole derivatives and related compounds were tested in vitro for possible anti-leishmanial activity against the promastigotes of L. donovani. Micromolar concentrations of these agents were used to study the inhibition of multiplication of L. donovani promastigotes. Seven compounds were identified with potential antigrowth agents of the parasite. Compound 4a was the most active at 50 μM followed by compound 3a. These compounds could prove useful as a future alternative for the control of visceral leishmaniasis.
杜氏利什曼原虫是内脏利什曼病的病原体,通过沙蝇传播,并在其哺乳动物宿主细胞内复制。抗药性菌株的出现阻碍了全球范围内控制疾病传播的努力。我们对 44 种 1,3,4-噻二唑衍生物和相关化合物进行了体外测试,以评估它们对杜氏利什曼原虫前鞭毛体的潜在抗利什曼活性。这些药物的微摩尔浓度用于研究抑制杜氏利什曼原虫前鞭毛体繁殖的效果。有七种化合物被鉴定为具有潜在抗寄生虫生长作用的物质。化合物 4a 在 50μM 时活性最高,其次是化合物 3a。这些化合物可能成为未来控制内脏利什曼病的一种替代方法。