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New N-phenylacetamide-incorporated 1,2,3-triazoles: [Et3NH][OAc]-mediated efficient synthesis and biological evaluation

机译:新的N-苯基乙酰胺掺入1,2,3-三唑:[ET3NH] [OAC]介导的有效合成和生物学评估

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A facile, highly efficient, and greener method for the synthesis of new 1,4-disubstituted-1,2,3-triazoles was conducted using [Et _(3) NH][OAc] as a medium by the implementation of ultrasound irradiation via click chemistry, affording excellent yields. The present synthetic method exhibited numerous advantages such as mild reaction conditions, excellent product yields, minimal chemical waste, operational simplicity, shorter reaction time, and a wide range of substrate scope. The synthesized compounds were further evaluated for in vitro antifungal activity against five fungal strains, and some of the compounds displayed equivalent or greater potency than the standard drug. A molecular docking study against the modelled three-dimensional structure of cytochrome P450 lanosterol 14α-demethylase was also performed to understand the binding affinity and binding interactions of the enzyme. Furthermore, the synthesized compounds were evaluated for DPPH radical scavenging activity and antitubercular activity against Mycobacterium tuberculosis H37Rv strain.
机译:通过实施超声辐射,使用[ET _(3)NH] [OAC]作为培养基进行了合成新的1,4-二取代-1,2,3-三唑的容易,高效和更环保的方法通过点击化学,提供出色的收益率。本发明的合成方法表现出许多优点,例如温和的反应条件,优异的产品产量,最小化学废物,操作简单,较短的反应时间和宽范围的基板范围。进一步评估合成化合物,用于对5个真菌菌株的体外抗真菌活性,以及​​一些化合物显示出比标准药物的等同物或更高的效力。还进行了针对细胞色素P450LANETTOL醇14α-脱甲基酶的模拟三维结构的分子对接研究,以了解酶的结合亲和力和结合相互作用。此外,评价合成化合物的DPPH自由基清除活性和针对结核分枝杆菌H37RV菌株的抗细胞活性。

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