Tiwari Avinash, Kumar Santosh, Shivahare Rahul, Kant Padam, Gupta Suman, Suryawanshi S N
Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
Bioorg Med Chem Lett. 2015 Jan 15;25(2):410-3. doi: 10.1016/j.bmcl.2014.09.078. Epub 2014 Oct 2.
Some novel heteroretinoid-bisbenzylidine ketone hybrids have been synthesized and evaluated for their in vitro antileishmanial activity against intramacrophagic amastigotes of Leishmania donovani. Among all the nine synthetic compounds, five compounds (7c, 7d and 7f-h) have shown significant (less than 7μM) activity against intramacrophagic amastigotes. The IC50 values of these compounds were found better than the reference drugs sodium stibogluconate (SSG) and miltefosine. This study helped us in identifying the new class of compounds that could be exploited as potent antileishmanial agents.
一些新型杂环视黄酸-双苄叉丙酮杂化物已被合成，并针对其对杜氏利什曼原虫巨噬细胞内无鞭毛体的体外抗利什曼活性进行了评估。在所有九种合成化合物中，有五种化合物（7c、7d和7f - h）对巨噬细胞内无鞭毛体显示出显著（小于7μM）活性。发现这些化合物的IC50值优于参考药物葡萄糖酸锑钠（SSG）和米替福新。这项研究有助于我们确定可作为强效抗利什曼原虫剂开发的新型化合物。
