Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow 226 001, India.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):291-3. doi: 10.1016/j.bmcl.2009.10.117. Epub 2009 Oct 30.
A series of aryloxy alkyl/aryl alkyl imidazoles were synthesized and evaluated in vitro as antileishmanials against Leishmania donovani. All the 19 compounds exhibited 94-100% inhibition at 10microg/mL against promastigotes and 12 compounds exhibited high inhibition with an IC(50) in the range of 0.47-4.85microg/mL against amastigotes. Promising compounds were tested further in vivo. Among all, compounds 4 and 23 with 4-CF(3) aryloxy moiety exhibited medium in vivo inhibition of 58-60%, thus providing new structural lead for antileishmanials.
一系列芳氧基烷基/芳基烷基咪唑类化合物被合成并进行了体外抗利什曼原虫活性评价，以检测其对利什曼原虫的抗药性。所有 19 种化合物在 10μg/mL 时对前鞭毛体的抑制率达到 94-100%，12 种化合物对无鞭毛体的抑制率较高，IC50 范围在 0.47-4.85μg/mL。有前途的化合物在体内进一步进行了测试。其中，具有 4-CF3 芳氧基部分的化合物 4 和 23 表现出中等的体内抑制率为 58-60%，因此为抗利什曼原虫药物提供了新的结构先导物。
