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Synthesis, characterization and biological evaluation of novel series of 2-(benzylamino)-2-oxoethyl]-2-oxo-2H-1-benzopyran-3-carboxamide derivatives
Indian Journal of Chemistry, Section B Pub Date : 2020-03-13
Mamata Devendra Naik, Yadav D Bodke, Ajeesh A K Kumar, Jayanth K Naik, Sudhesh L Shastri

A novel series of benzopyran-3-carboxamide derivatives have been designed and synthesized using a smooth and linear multistep synthesis. Amidation of coumarin-3-carboxylic acid with glycine ethyl ester in the presence of EDC.HCl and HOBt as coupling agent followed by the hydrolysis results in the formation of key synthon, [(2-oxo-2H-1-benzopyran-3-carbonyl) amino] acetic acid 7 which is further coupled with substituted aryl amines using HATU in combination with Hünig’s base to get the target compounds 8(a-h). The synthesized compounds have been screened for their in vitro antibacterial and antioxidant activity and the results are expressed as MIC and IC50 values respectively. Further, the binding ability of synthesized compounds with different proteins have been examined by molecular docking studies.

中文翻译:

新型2-(苄氨基)-2-氧代乙基] -2-氧代-2H-1-苯并吡喃-3-羧酰胺衍生物的合成,表征及生物学评价

已经设计了一系列新颖的苯并吡喃-3-甲酰胺衍生物,并使用平滑且线性的多步合成方法进行了合成。在EDC.HCl和HOBt作为偶联剂存在下,用甘氨酸乙酯酰胺化香豆素-3-羧酸,然后水解,形成关键的合成子[(2-oxo-2 H -1-benzopyran-3 -羰基)氨基]乙酸7,进一步使用HATU与Hünig碱组合与取代的芳基胺偶联,得到目标化合物8(ah)。筛选了合成的化合物的体外抗菌和抗氧化活性,结果表示为MIC和IC 50值。此外,已经通过分子对接研究检查了合成化合物与不同蛋白质的结合能力。
更新日期:2020-03-13
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