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

Article

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

Shaopeng Wei, Wenjun Wu and Zhiqin Ji*

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; in revised form: 24 March 2012 / Accepted: 6 April 2012 / Published: 16 April 2012

(This article belongs to the Section Bioactives and Nutraceuticals)

Download PDF Full-Text [229 KB, uploaded 16 April 2012 14:35 CEST]

Abstract: 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

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