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Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2011-07-27 , DOI: 10.1016/j.ejmech.2011.07.033
K.D. Thomas , Airody Vasudeva Adhikari , Sandeep Telkar , Imran H. Chowdhury , Riaz Mahmood , Nishith K. Pal , Guru Row , E. Sumesh

Three new series of 4-hydroxy-8-trifluoromethyl-quinoline derivatives were synthesized through multi step reactions. All the newly synthesized compounds were characterized by spectral and elemental analyses. The structure of 5j was evidenced by X-ray crystallographic study. The newly synthesized title compounds were evaluated for their antimicrobial activities including antimycobacterial activity. Amongst the tested compounds, 5b, 5e, 5h, 5j, 6c and 7c displayed promising antimicrobial activity. The mode of action of these active compounds was carried out by docking of receptor enoyl-ACP reductase with newly synthesized candidate ligands, 5b, 5e, 5h, 5j and 6c.



中文翻译:

新的喹啉-3-碳酰肼衍生物作为抗结核药的设计,合成和对接研究

通过多步反应合成了三个新的4-羟基-8-三氟甲基-喹啉衍生物系列。所有新合成的化合物都通过光谱和元素分析进行​​了表征。X射线晶体学研究证明了5j的结构。评价新合成的标题化合物的抗微生物活性,包括抗分枝杆菌活性。在测试的化合物中,5b5e5h5j6c7c显示出有希望的抗菌活性。这些活性化合物的作用方式是通过将受体烯酰-ACP还原酶与新合成的候选配体5b对接来进行的5e5h5j6c

更新日期:2011-07-27
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