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用于抗菌活性的 N-取代咪唑衍生物的合成与评价

Synthesis and Evaluation of N-substituted Imidazole Derivatives for Antimicrobial Activity.

作者信息

Gupta Namita, Pathak D P

机构信息

Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR), Sector-3, Pushp Vihar, New Delhi-110 017, India.

出版信息

Indian J Pharm Sci. 2011 Nov;73(6):674-8. doi: 10.4103/0250-474X.100246.

Abstract

A series of N-substituted imidazole derivatives was synthesized. Imidazole nucleus was reacted with ethylchloroacetate to form imidazole ester. Reaction of the imidazole ester (I) with different amines yields the desired products (1a- 1e). The compounds were characterized by FT-IR, (1)H-NMR and mass spectra. The synthesized compounds were evaluated for the antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger by determination of MIC (minimum inhibitory concentration) using tube dilution method. Compound (1b) was found to be the most active antimicrobial compound amongst others in the series.

摘要

合成了一系列N-取代咪唑衍生物。咪唑核与氯乙酸乙酯反应形成咪唑酯。咪唑酯(I)与不同的胺反应得到所需产物(1a - 1e)。通过傅里叶变换红外光谱(FT-IR)、氢核磁共振谱(¹H-NMR)和质谱对这些化合物进行了表征。采用试管稀释法测定最低抑菌浓度(MIC),对合成的化合物针对金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌、铜绿假单胞菌、白色念珠菌和黑曲霉的抗菌活性进行了评估。发现化合物(1b)是该系列中最具活性的抗菌化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7e82/3480755/c6d62dda73ef/IJPhS-73-674-g001.jpg

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