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2-羟基丙酸衍生物的合成、抗菌活性评价及定量构效关系研究

Synthesis, antimicrobial evaluation and QSAR studies of 2-hydroxy propanoic acid derivatives.

作者信息

Bansal A, Kumar P, Narasimhan B

机构信息

Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India.

出版信息

Drug Res (Stuttg). 2014 May;64(5):240-5. doi: 10.1055/s-0033-1357127. Epub 2013 Oct 8.

Abstract

A series of 2-hydroxypropanoic acid derivatives (1-26) was synthesized and characterized by physicochemical and spectral means. The synthesized compounds were evaluated for their in vitro antimicrobial potential and the results indicated that compounds 5 and 12 were found to be the most potent antimicrobial agents having pMICam values 1.67 and 1.64 µM/ml respectively. QSAR studies indicated the importance of topological parameter, Kier's valance second order molecular connectivity index (2χv) in describing the antimicrobial activities of synthesized 2-hydroxypropanoic acid derivatives.

摘要

合成了一系列2-羟基丙酸衍生物(1-26),并通过物理化学和光谱手段对其进行了表征。对合成的化合物进行了体外抗菌潜力评估,结果表明化合物5和12是最有效的抗菌剂,其pMICam值分别为1.67和1.64μM/ml。定量构效关系(QSAR)研究表明,拓扑参数——基尔价二阶分子连接性指数(2χv)在描述合成的2-羟基丙酸衍生物的抗菌活性方面具有重要意义。

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