期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 13, 期 4, 页码 4819-4830出版社
MDPI AG
DOI: 10.3390/ijms13044819
关键词
benzimidazolone (thione) derivatives; synthesis; antibacterial activity
资金
- Science and Technology Ministry of China [2010CB126100]
- National Natural Science Foundation of China [30971935]
- Education Ministry of China
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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