1,2 -二取代苯并咪唑的合成、表征及抗菌研究

K. Girija, S. Indhumathi
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引用次数: 0

摘要

以邻苯二胺与不同芳香醛在硝酸铈铵存在下缩合生成2-取代苯并咪唑,再与仲胺和甲醛缩合生成1,2 -二取代苯并咪唑。用薄层色谱法检测合成化合物的纯度,并用FT-IR、1HNMR、质谱分析对其进行了表征。与标准环丙沙星相比,该化合物对枯草芽孢杆菌具有中等抑菌活性,对大肠杆菌具有良好的抑菌活性。合成的两种化合物3a[(2-{[2-(3-氯苯基)- 1h -苯并咪唑-1-基]甲基}- 1h -异吲哚- 1,3 (2H)-二酮]和5a[2-{[2-(2-氯苯基)- 1h -苯并咪唑-1-基]甲基}- 1h -异吲哚- 1,3 (2H)-二酮]的抗结核活性检测显示对结核分枝杆菌(H37Rv)具有显著的抗结核活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, Characterization and Antimicrobial Study of 1, 2-Disubstituted Benzimidazoles
A series of novel disubstituted benzimidazole derivatives were synthesized by condensation of o-phenylenediamine with different aromatic aldehydes in presence of ceric ammonium nitrate forming 2-substituted benzimidazoles which on further condensation with secondary amine and formaldehyde forms 1, 2-disubstituted benzimidazoles. The purity of the synthesized compounds was monitored by thin layer chromatography and characterized by FT-IR, 1HNMR, MASS spectral analysis. The compound exhibited moderate antibacterial activity against Bacillus subtilis, good activity against Escherichia coli, compared to standard ciprofloxacin. The two synthesized compounds named 3a [ (2-{[2-(3-chlorophenyl)-1H-benzimidazol-1-yl] methyl}-1H-isoindole-1, 3(2H)-dione)] and 5a [2-{[2-(2-chlorophenyl)-1H-benzimidazol-1-yl] methyl}-1H-isoindole-1, 3(2H)-dione] were tested for the antitubercular activity showed a significant activity against Mycobacterium tuberculosis (H37Rv).
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