Vanillin-tethered quinazolin-2,4-dione analogues through five- and/or six-membered nitrogen-containing heterocycles as antibacterial agents: synthesis, biological evaluation and molecular docking study.

ABSTRACT: The escalating threat of drug-resistant bacteria confirms the urgent need to develop and identify new and potent antibacterial inhibitors. In the present research study, the molecular hybridization strategy involved the synthesis of vanillin linked to a quinazolin-2,4-dione skeleton through five- and/or six-membered nitrogen-containing heterocycles such as pyrazole, isoxazole and/or pyrimidine 1-15 and testing them for their in vitro antibacterial studies. The vanillin-derived chalcone 1 was synthesized by treatment of 3-(4-acetyl-phenyl)-1H-quinazolin-2,4-dione with 4-hydroxy-3-methoxybenzaldehyde (vanillin) through a base-catalyzed Claisen-Schmidt condensation reaction, then used as a key precursor for synthesis of a series of 14 bioactive compounds 2-15 by treatment with n

SUBMITTER: Abdelmonsef AH 

PROVIDER: S-EPMC12836203 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature