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Int. J. Mol. Sci. 2012, 13(4), 4819-4830; doi:10.3390/ijms13044819

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

College of plant protection and Institute of Pesticide Science, Northwest A & F University, Shaanxi 712100, China
* Author to whom correspondence should be addressed.
Received: 7 March 2012 / Revised: 24 March 2012 / Accepted: 6 April 2012 / Published: 16 April 2012
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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A series of (28) 1-alkyl-3-methacryloyl (acryloyl)-benzimidazolone (thione) deriv-atives were synthesized. The structures of the new derivatives were confirmed by 1H-NMR, 13C-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.
Keywords: benzimidazolone (thione) derivatives; synthesis; antibacterial activity benzimidazolone (thione) derivatives; synthesis; antibacterial activity
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Wei, S.; Wu, W.; Ji, Z. Synthesis and Antibacterial Activities of 1-Alkyl-3-methacryloyl (Acryloyl) of Benzimidazolone (Thione) Derivatives. Int. J. Mol. Sci. 2012, 13, 4819-4830.

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