新型四氢萘唑和相关环己基唑类化合物的设计与合成作为抗利什曼原虫药物。
Design and synthesis of novel tetrahydronaphthyl azoles and related cyclohexyl azoles as antileishmanial agents.
机构信息
Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow, India.
出版信息
Bioorg Med Chem Lett. 2011 Mar 1;21(5):1407-10. doi: 10.1016/j.bmcl.2011.01.026. Epub 2011 Jan 11.
A novel series of trans-2-aryloxy-1,2,3,4,-tetrahydronaphthyl azoles and related cyclohexyl azoles were synthesized and evaluated in vitro against Leishmania donovani. Compound 9 identified as most active analog with IC(50) value of 0.64 μg/mL and SI value of 34.78 against amastigotes, and is several folds more potent than the reference drugs sodium stilbogluconate and paromomycin. It also exhibited significant in vivo inhibition of 83.33%, and provided a new structural scaffold for antileishmanials.
新型系列反式-2-芳氧基-1,2,3,4-四氢萘基氮唑和相关环己基氮唑被合成并在体外对杜氏利什曼原虫进行评估。化合物 9 被鉴定为最具活性的类似物，对前鞭毛体的 IC50 值为 0.64μg/mL，SI 值为 34.78，比参考药物葡萄糖酸钠和巴龙霉素的效力高出数倍。它还表现出对 83.33%的显著体内抑制作用，并为抗利什曼原虫药物提供了新的结构支架。
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