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Synthesis and evaluation of novel triazolyl quinoline derivatives as potential antileishmanial agents
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2018-05-12 , DOI: 10.1016/j.ejmech.2018.05.014
Akanksha Upadhyay , Pragati Kushwaha , Sampa Gupta , Ranga Prasad Dodda , Karthik Ramalingam , Ruchir Kant , Neena Goyal , Koneni V. Sashidhara

The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2.43 to 45.75 μM) and intracellular amastigotes (IC50 ranging from 7.06 to 34.9 μM) than the control, miltefosine (IC50 = 8.4 μM), with less cytotoxicity in comparison to the standard drugs. Overall results revealed that prototype signify a new structural lead for antileishmanial chemotherapy.



中文翻译:

新型三唑基喹啉衍生物作为潜在的抗疟药的合成与评价

含喹啉的天然产物及其衍生物在药物化学中的巨大潜力使我们发现了一系列25种化合物,用于开发新的抗疟药。通过点击化学启发的分子杂交方法合成了一系列三唑基2-甲基-4-苯基喹啉-3-羧酸酯衍生物,并针对利什曼原虫进行了评估。大部分的筛选衍生物表现出显著体外抗利什曼病活性对前鞭毛体(IC 50范围从2.43到45.75μM)和胞内无鞭毛体(IC 50范围从7.06至34.9μM)比对照,米替福新(IC 50 = 8.4μM),与标准药物相比,细胞毒性较小。总体结果表明,原型标志着抗衰老化学疗法的新结构领先。

更新日期:2018-05-12
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