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Synthesis of Coumarins Coupled with Benzamides as Potent Antimicrobial Agents
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2020-09-01 , DOI: 10.1007/s11094-020-02245-4
Muthipeedika Nibin Joy , Vasiliy A. Bakulev , Yadav D. Bodke , Sandeep Telkar

A series of new coumarin derivatives coupled with benzamides have been synthesized and screened for their antimicrobial properties. Some compounds displayed promising antibacterial activity (MIC ranging within 5 – 150 μg/mL) and moderate antifungal activity as compared to the respective standards. Compounds 6p, 6l and 6m displayed promising antibacterial activity comparable with the standard drug ciprofloxacin, and compound 6m exhibited better antifungal activity in comparison to other synthesized compounds. In silico docking studies of the active compounds were carried out against the gyrase enzyme, and it was concluded that compound 6p exhibited significant hydrogen bonding and hydrophobic interactions which could be the plausible reason for its superior activity as compared to the other synthesized compounds.

中文翻译:

合成香豆素联用苯甲酰胺作为强效抗菌剂

已经合成了一系列与苯甲酰胺偶联的新香豆素衍生物并筛选了它们的抗菌特性。与各自的标准相比,一些化合物显示出有希望的抗菌活性(MIC 在 5 – 150 μg/mL 范围内)和中等抗真菌活性。化合物 6p、6l 和 6m 显示出与标准药物环丙沙星相当的有希望的抗菌活性,与其他合成化合物相比,化合物 6m 显示出更好的抗真菌活性。针对促旋酶对活性化合物进行了计算机对接研究,得出的结论是化合物 6p 表现出显着的氢键和疏水相互作用,这可能是其与其他合成化合物相比具有优异活性的合理原因。
更新日期:2020-09-01
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