SYNTHESIS AND IN VITRO ANTIMICROBIAL EVALUATION OF PIPERAZINE SUBSTITUTED QUINAZOLINE-BASED THIOUREA/THIAZOLIDINONE/CHALCONE HYBRIDS

摘要

In frames of the search for new biological entities to fight against recent drug-resistant microbial strains, we report a library of quinazoline-based thiourea/4-thiazolidinone/chalcone hybrids. The newly synthesized compounds were studied for efficacy against several bacteria {Staphylococcus aureus. Bacillus cereus, Pseudomonas aeruginosa, and Klebsiella pneumoniae) and fungi (Candida albicans and Aspergillus clavatus) using the broth dilution technique. From the biological evaluation, (E)-3-(3,4-dimethoxyphenyl)-l-(4-((4-(4-ethylpiperazin-1 -yl)quinazolin-2-yl)amino)phenyl)prop-2-en-1 -onewas found to be the most active analogue (microbial inhibition concentration 3.12 ug/mL) to inhibit the bacterial growth. The rest of the compounds showed equipotent efficacy (3.12—12.5 ug/mL) as compared to the standard. Final compounds were characterized by FT-IR, 'H NMR, ~(l3)C NMR, mass spectroscopy, and elemental analysis.