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Title: | Study of benzofuroquinolinium derivatives as a new class of potent antibacterial agent and the mode of inhibition targeting FtsZ | Authors: | Zheng, YY Du, RL Cai, SY Liu, ZH Fang, ZY Liu, T So, LY Lu, YJ Sun, N Wong, KY |
Issue Date: | 2018 | Source: | Frontiers in microbiology, 17 Aug. 2018, v. 9, 1937 | Abstract: | New generation of antibacterial agents are urgently needed in order to fight the emergence of multidrug-resistant bacteria. FtsZ is currently identified as a promising target for new types of antimicrobial compounds development because of its conservative characteristics and its essential role played in bacterial cell division. In the present study, the antibacterial activity of a series of benzofuroquinolinium derivatives was investigated. The results show that the compounds possess potent antibacterial activity against drug resistant pathogens including MRSA, VREF and NDM-1 Escherichia coli. Biological studies reveal that the compound is an effective inhibitor that is able to suppress FtsZ polymerization and GTPase activity and thus stopping the cell division and causing cell death. More importantly, this series of compounds shows low cytotoxicity on mammalian cells and therefore they could be new chemotypes for the development of new antibacterial agents targeting the cell-division protein FtsZ. | Keywords: | Bacterial resistance Antibacterial activity Cell division FtsZ inhibitor FtsZ polymerization |
Publisher: | Frontiers Research Foundation | Journal: | Frontiers in microbiology | ISSN: | 1664-302X | DOI: | 10.3389/fmicb.2018.01937 | Rights: | Copyright © 2018 Zheng, Du, Cai, Liu, Fang, Liu, So, Lu, Sun and Wong. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. The following publication Zheng Y-Y, Du R-L, Cai S-Y, Liu Z-H, Fang Z-Y, Liu T, So L-Y, Lu Y-J, Sun N and Wong K-Y (2018) Study of Benzofuroquinolinium Derivatives as a New Class of Potent Antibacterial Agent and the Mode of Inhibition Targeting FtsZ. Front. Microbiol. 9:1937 is available at https://dx.doi.org/10.3389/fmicb.2018.01937 |
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