Abstract
A series of novel 3-O-arylalkylbenzamide derivatives as FtsZ inhibitors was designed, synthesized and evaluated for their cell division inhibitory activity against B. subtilis and S. aureus, and in vitro antibacterial activity against various phenotypes of Gram-positive bacteria. This series showed significantly improved on-target activity and in vitro antibacterial activity compared with 3-MBA. Among them, 3-O-alkylbenzamids 4–8 and 3-O-bromoalkylbenzamides 9 and 10 showed significantly improved activity against three phenotypes of S. aureus ATCC25923, S. aureusATCC29213 (MRSA) and S. aureus PR. Preliminary structure-activity relationships indicated that the extension of 3-O-alkyl side chain resulted in a substantial improvement in the antibacterial activity, and the small group like methyl or ethyl group at the position 1–3 of the 3-O-alkyl side chain did not affect the antibacterial activity while the large group such as benzene or heterocycle at the position 4 or 5 of the 3-O-alkyl side chain could lead to poor antibacterial activity.
Keywords: Antibacterial evaluation, 3-O-Arylalkyl groups, Benzamide derivatives, FtsZ inhibitors, Resistant bacteria, Synthesis
Letters in Drug Design & Discovery
Title:The Synthesis and Antibacterial Activity of Novel 3-O-arylalkylbenzamide Derivatives as FtsZ Inhibitors
Volume: 10 Issue: 4
Author(s): Siti Ma, Rongmei Wang, Yuanze Wang, Jichao Cao and Shutao Ma
Affiliation:
Keywords: Antibacterial evaluation, 3-O-Arylalkyl groups, Benzamide derivatives, FtsZ inhibitors, Resistant bacteria, Synthesis
Abstract: A series of novel 3-O-arylalkylbenzamide derivatives as FtsZ inhibitors was designed, synthesized and evaluated for their cell division inhibitory activity against B. subtilis and S. aureus, and in vitro antibacterial activity against various phenotypes of Gram-positive bacteria. This series showed significantly improved on-target activity and in vitro antibacterial activity compared with 3-MBA. Among them, 3-O-alkylbenzamids 4–8 and 3-O-bromoalkylbenzamides 9 and 10 showed significantly improved activity against three phenotypes of S. aureus ATCC25923, S. aureusATCC29213 (MRSA) and S. aureus PR. Preliminary structure-activity relationships indicated that the extension of 3-O-alkyl side chain resulted in a substantial improvement in the antibacterial activity, and the small group like methyl or ethyl group at the position 1–3 of the 3-O-alkyl side chain did not affect the antibacterial activity while the large group such as benzene or heterocycle at the position 4 or 5 of the 3-O-alkyl side chain could lead to poor antibacterial activity.
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Cite this article as:
Ma Siti, Wang Rongmei, Wang Yuanze, Cao Jichao and Ma Shutao, The Synthesis and Antibacterial Activity of Novel 3-O-arylalkylbenzamide Derivatives as FtsZ Inhibitors, Letters in Drug Design & Discovery 2013; 10 (4) . https://dx.doi.org/10.2174/1570180811310040005
DOI https://dx.doi.org/10.2174/1570180811310040005 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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