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Antibacterial activity evaluation and mode of action study of novel thiazole-quinolinium derivatives

Ying Li, Ning Sun, Hooi‐Leng Ser, Wei Long, Yanan Li, Cuicui Chen, Bo‐Xin Zheng, Xuan‐He Huang, Zhihua Liu, Yu‐Jing Lu

2020RSC Advances41 citationsDOIOpen Access PDF

Abstract

. Furthermore, compounds 4a1-4a4 and 4b1-4b4 altered the morphology of bacterial cells and the cells displayed a more-elongated shape compared to the untreated cells. Biochemical assays showed that 4a4 and 4b4 stimulate FtsZ polymerization in bacterial cells, which eventually disrupts its dynamic assembly and Z-ring formation. The inhibition of this crucial step in bacterial cell division could potentially represent their main mechanism of antibacterial activity. Cytotoxicity assay and hemolysis assay suggested that 4a4 and 4b4 possess low cytotoxicity. In summary, these results further highlight the importance of 4a4 and 4b4 that could be developed as potent and effective bacteriostatic agents against multi-drug resistant bacteria.

Topics & Concepts

ThiazoleAntibacterial activityCombinatorial chemistryChemistryMode of actionAction (physics)StereochemistryBiochemistryBiologyPhysicsBacteriaGeneticsQuantum mechanicsSynthesis and Biological EvaluationSynthesis and biological activityPhenothiazines and Benzothiazines Synthesis and Activities
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