Synthesis and Antibacterial Activities of 1-Alkyl-3-methacryloyl (Acryloyl) of Benzimidazolone (Thione) Derivatives

被引：15

作者：

Wei, Shaopeng

Wu, Wenjun

Ji, Zhiqin ^{[1
]}

机构：

[1] NW A&F Univ, Coll Plant Protect, Yangling 712100, Shaanxi, Peoples R China

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2012年 / 13卷 / 04期

基金：

中国国家自然科学基金;

关键词：

benzimidazolone (thione) derivatives; synthesis; antibacterial activity; DISCOVERY; AGONISTS;

D O I：

10.3390/ijms13044819

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of (28) 1-alkyl-3-methacryloyl (acryloyl)-benzimidazolone (thione) deriv-atives were synthesized. The structures of the new derivatives were confirmed by H-1-NMR, C-13-NMR and ESI-MS spectral analysis. The antibacterial activities of these compounds against several strains of bacteria, such as Bacillus cereus, Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, were evaluated by methods of paper disc-diffusion and broth mciro-dilution. Methacryloyl derivatives displayed higher antibacterial activities against tested bacterial strains than those of acryloyl derivatives in in vitro tests. A structure-activity relationship (SAR) study revealed that the presences of the methacryloyl moieties is essential to the antibacterial activities of the compounds.

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收藏

页码：4819 / 4830

页数：12

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