4.6 Article

The study of 9,10-dihydroacridine derivatives as a new and effective molecular scaffold for antibacterial agent development

期刊

出版社

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bbrc.2021.01.096

关键词

FtsZ inhibitor; Drug-resistant strain; Antibacterial activity; 9; 10-Dihydroacridine derivative br

资金

  1. National Natural Science Foundation of China [81700076, 81473082]
  2. Nature Science Foundation of Guangdong Province, China [2017A0 30313078, 2017A030313071, 2019A1515011799]
  3. Department of Agriculture and Rural Affairs of Guangdong Province, China [2018LM2175]
  4. Science and Technology Planning Project of Guangdong Province [2017A010103044]
  5. Jiangmen Program for Innovative Research Team [2018630100180019806]

向作者/读者索取更多资源

The study revealed that two 9,10-dihydroacridine derivatives have strong antibacterial activity against selected Gram-positive bacteria by promoting FtsZ polymerization and disrupting Z-ring formation, leading to bacterial cell division interruption and cell death.
The emergence of worldwide spreading drug-resistant bacteria has been a serious threat to public health during the past decades. The development of new and effective antibacterial agents to address this critical issue is an urgent action. In the present study, we investigated the antibacterial activity of two 9,10-dihydroacridine derivatives and their mechanism. Both compounds were found possessing strong antibacterial activity against some selected Gram-positive bacteria including MRSA, VISA and VRE. The biological study suggests that the compounds promoted FtsZ polymerization and also disrupted Z-ring formation at the dividing site and consequently, the bacterial cell division is interrupted and causing cell death. (c) 2021 Elsevier Inc. All rights reserved.

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