Synthesis of Novel Quinazolinone Analogues for Quorum Sensing Inhibition.

ABSTRACT: As bacteria continue to develop resistance mechanisms against antimicrobials, an alternative method to tackle this global concern must be developed. As the pqs system is the most well-known and responsible for biofilm and pyocyanin production, quinazolinone inhibitors of the pqs system in P. aeruginosa were developed. Molecular docking following a rationalised medicinal chemistry approach was adopted to design these analogues. An analysis of docking data suggested that compound 6b could bind with the key residues in the ligand binding domain of PqsR in a similar fashion to the known antagonist M64. The modification of cyclic groups at the 3-position of the quinazolinone core, the introduction of a halogen at the aromatic core and the modification of the terminal

SUBMITTER: Shandil S 

PROVIDER: S-EPMC10376653 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature