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首页> 外文期刊>European journal of pharmaceutical sciences >Synthesis, In silico studies and In vitro evaluation for antioxidant and antibacterial properties of diarylmethylamines: A novel class of structurally simple and highly potent pharmacophore
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Synthesis, In silico studies and In vitro evaluation for antioxidant and antibacterial properties of diarylmethylamines: A novel class of structurally simple and highly potent pharmacophore

机译:二芳基甲胺的抗氧化剂和抗菌性能的合成,计算机模拟研究和体外评估:一类结构简单且高效的药效基团

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摘要

A series of novel diarylmethylamines were synthesized via simple three component condensation reaction. In vitro antibacterial activity of the synthesized compounds was assessed against Gram-positive and Gram-negative bacteria. Compound 1f containing phenyl and N-methyl piperazine moiety was found to be potent against both pathogenic bacteria with MIC value of 31 mu g/mL. Diarylmethylamine 1l containing sesamol and N-methyl piperazine units was found to be the most effective against Gram-positive bacteria with MIC value of 15 mu g/mL. The compound leads to the damage of the bacterial cell membrane which was demonstrated by flow cytometry (FC) and field emission scanning electron microscopy (FESEM). Radical scavenging activity of compounds 1l and 1m was found out to be comparable with that of standard antioxidant BHT. Further, in silico studies were carried out to calculate the physico-chemical parameter of the synthesized compounds. (C) 2016 Elsevier B.V. All rights reserved.
机译:通过简单的三组分缩合反应合成了一系列新颖的二芳基甲胺。评估了合成化合物对革兰氏阳性和革兰氏阴性细菌的体外抗菌活性。发现含有苯基和N-甲基哌嗪部分的化合物1f对两种病原菌均有效,MIC值为31μg/ mL。含有芝麻酚和N-甲基哌嗪单元的二芳基甲胺1l被发现对革兰氏阳性细菌最有效,MIC值为15μg / mL。该化合物导致细菌细胞膜受损,这通过流式细胞仪(FC)和场发射扫描电子显微镜(FESEM)得以证明。发现化合物1l和1m的自由基清除活性与标准抗氧化剂BHT相当。此外,进行了计算机模拟研究以计算合成化合物的物理化学参数。 (C)2016 Elsevier B.V.保留所有权利。

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