Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents
Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents
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DOI：
10.1016/j.bmcl.2017.07.008
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发表时间：
2017-08-15
影响因子：
2.7
通讯作者：
Sarma, Diganta
中科院分区：
文献类型：
--
作者：
Ali, Abdul Aziz;Gogoi, Dhrubajyoti;Sarma, Diganta
采用流行的“点击化学”方法高效合成了17个新型1,2,3-三唑衍生物，并体外评价了它们对结核分枝杆菌H37Ra的抗结核活性。在这些化合物中，6种化合物表现出显著的活性，最小抑制浓度（MIC）值在3.12 ~ 0.78 μ g/mL之间，并且对小鼠骨髓源性巨噬细胞（MBMDMQs）没有明显的细胞毒性。目标化合物与DprEl （decaprenylphospyl - β - d -核糖-2'-epimerase）酶活性位点的分子对接揭示了可能的结合相互作用的重要信息。(C) 2017 Elsevier Ltd.版权所有。
A library of seventeen novel 1,2,3-triazole derivatives were efficiently synthesized in excellent yields by the popular 'click chemistry' approach and evaluated in vitro for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra (ATCC 25177 strain). Among the series, six compounds exhibited significant activity with minimum inhibitory concentration (MIC) values ranging from 3.12 to 0.78 mu g/mL and along with no significant cytotoxicity against MBMDMQs (mouse bone marrow derived macrophages). Molecular docking of the target compounds into the active site of DprEl (Decaprenylphosphoryl-beta-D-ribose-2'-epimerase) enzyme revealed noteworthy information on the plausible binding interactions. (C) 2017 Elsevier Ltd. All rights reserved.