Synthesis and antibiofilm evaluation of 3-hydroxy-2,3-dihydroquinazolin-4(1H)-one derivatives against opportunistic pathogen Acinetobacter baumannii.

Bioorg Med Chem

State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, School of Pharmacy, Guizhou Medical University, Guiyang 550004, China. Electronic address:

Published: August 2020

AI Article Synopsis

  • The rise of multidrug-resistant microorganisms has led researchers to explore new antimicrobial approaches, focusing on antivirulence strategies to reduce drug resistance.
  • A total of 22 quorum sensing inhibitors were created by mimicking the structure of certain natural compounds.
  • One inhibitor showed a 34% reduction in biofilm formation and enhanced the effectiveness of Gentamycin sulfate by inhibiting extracellular polysaccharides.

Article Abstract

The emergence of multidrug resistant microorganisms has triggered the impending need for new aitimicrobial strategies. The antivirulence strategy with the benefite of alleviating the drug resistance becomes the focus of research. In this study, 22 quorum sensing inhibitors were synthesized by mimicking the structure of autoinducer and acinetobactin and up to 34% biofilm inhibition was observed with 5u. The biofilm inhibition effect was further demonstrated with extracellular polysaccharides inhibition and synergism with Gentamycin sulphate.

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Source
http://dx.doi.org/10.1016/j.bmc.2020.115606DOI Listing

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