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Title: A thiazole orange derivative targeting the bacterial protein FtsZ shows potent antibacterial activity
Authors: Sun, N 
Lu, YJ
Chan, FY 
Du, RL 
Zheng, YY
Zhang, K
So, LY 
Abagyan, R
Zhuo, C
Leung, YC 
Wong, KY 
Keywords: Bacterial resistance
Antibacterial activity
Cell division
FtsZ inhibitor
FtsZ polymerization
Issue Date: 2017
Publisher: Frontiers Research Foundation
Source: Frontiers in microbiology, 2017, v. 8, 855 How to cite?
Journal: Frontiers in microbiology 
Abstract: The prevalence of multidrug resistance among clinically significant bacteria calls for the urgent development of new antibiotics with novel mechanisms of action. In this study, a new small molecule exhibiting excellent inhibition of bacterial cell division with potent antibacterial activity was discovered through cell-based screening. The compound exhibits a broad spectrum of bactericidal activity, including the methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and NDM-1 Escherichia coli. The in vitro and in vivo results suggested that this compound disrupts the dynamic assembly of FtsZ protein and Z-ring formation through stimulating FtsZ polymerization. Moreover, this compound exhibits no activity on mammalian tubulin polymerization and shows low cytotoxicity on mammalian cells. Taken together, these findings could provide a new chemotype for development of antibacterials with FtsZ as the target.
ISSN: 1664-302X
DOI: 10.3389/fmicb.2017.00855
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