Synthesis, Structure Elucidation and Biological Activities of Some Novel 4(3H)-Quinazolinones as Anti-Biofilm Agents


Turk S., KARAKUŞ S., Ece A., ULUSOY S., Bosgelmez-Tinaz G.

LETTERS IN DRUG DESIGN & DISCOVERY, vol.16, no.3, pp.313-321, 2019 (Peer-Reviewed Journal) identifier identifier

  • Publication Type: Article / Article
  • Volume: 16 Issue: 3
  • Publication Date: 2019
  • Doi Number: 10.2174/1570180815666180621101123
  • Journal Name: LETTERS IN DRUG DESIGN & DISCOVERY
  • Journal Indexes: Science Citation Index Expanded, Scopus
  • Page Numbers: pp.313-321
  • Keywords: 4(3H)-Quinazolinones, structure elucidation, LasR protein, Pseudomonas aeruginosa, quorum sensing, biofilm formation, QUORUM-SENSING INHIBITORS, PSEUDOMONAS-AERUGINOSA, SWARMING MOTILITY, ACCURATE DOCKING, VIRULENCE, LIGAND, GLIDE, DERIVATIVES, PROTEIN

Abstract

Background: Pseudomonas aeruginosa is an opportunistic pathogen that causes chronic infections in immunocompromised patients. The inhibition of Quorum Sensing (QS) system has been recognized as an attractive strategy for the treatment of P. aeruginosa infections. In the present study, a series of novel 2-methyl-3[4-(substituedaminosulfonyl)phenyl]-4(3H)-quinazolinones (1-8) were synthesized and tested for their biofilm formation and swarming motility inhibitory activities in P. aeruginosa PA01.