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Int. J. Mol. Sci. 2013, 14(4), 6790-6804; doi:10.3390/ijms14046790
Article

Synthesis of 1-isopropyl-3-acyl-5-methyl-benzimidazolone Derivatives and Their Antimicrobial Activity

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,
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 and *
College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China
* Author to whom correspondence should be addressed.
Received: 22 January 2013 / Revised: 6 March 2013 / Accepted: 8 March 2013 / Published: 26 March 2013
(This article belongs to the Section Bioactives and Nutraceuticals)
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Abstract

A series of N-acylated analogues of 1-isopropyl-3-acyl-5-methyl-benzimidazolone were synthesized. Bioassay results indicated that analogues 5-07 and 5-19 exhibited the most potency against Bacillus cereus, Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Analogues 5-02, 5-07, 5-12, 5-15, 5-19, 5-20 and 5-25 could effectively inhibit the spore germination of Botrytis cinerea. The relationship between structure and their antimicrobial activity (SAR) has also been discussed according to aliphatic acids and aromatic acids derivatives, respectively. This implied that the N-acylated derivatives of 5-methyl-benzimidazolone might be potential antimicrobial agents.
Keywords: 5-methyl-benzimidazolone; N-acylated derivatives; antimicrobial activity 5-methyl-benzimidazolone; N-acylated derivatives; antimicrobial activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Xu, N.; Yang, C.; Gan, X.; Wei, S.; Ji, Z. Synthesis of 1-isopropyl-3-acyl-5-methyl-benzimidazolone Derivatives and Their Antimicrobial Activity. Int. J. Mol. Sci. 2013, 14, 6790-6804.

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