Highly Regioselective Ring-Opening of Epoxides: Synthesis and Biological Evaluation as Potent Antimicrobial Agents

N. H. Lalavani, K. A. Bhensdadia, S. Baluja
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Abstract

In present work, a convenient method for the nucleophilic ring-opening of epoxides with secondary amine in presence of ethyl acetate as a polar aprotic solvent using catalytic amount of base is described. Present method is highly regioselective and furnishes the products in short time of period with excellent yield. The regioselectivity of this ring opening was confirmed using FT-IR, 1H NMR, 13C NMR, elemental analysis and mass spectral data. The antimicrobial screening of all these synthesized compounds was done against some bacterial and fungal strains in two polar solvents, DMSO and DMF using agar well diffusion method. These compounds showed good inhibition of bacterial strains and potent against fungal strains than standard drug.
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高区域选择性开环环氧化物:作为有效抗菌剂的合成和生物学评价
本文介绍了一种在醋酸乙酯为极性非质子溶剂存在下,利用碱的催化量,用仲胺催化环氧化合物的亲核开环的简便方法。该方法具有较高的区域选择性,在较短的时间内可获得较高的收率。利用FT-IR、1H NMR、13C NMR、元素分析和质谱数据证实了该开环的区域选择性。采用琼脂孔扩散法在DMSO和DMF两种极性溶剂中对细菌和真菌进行了抗菌筛选。与标准药物相比,这些化合物对细菌有良好的抑制作用,对真菌有较强的抑制作用。
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