Efficient one pot synthesis of xanthene-triazole-quinoline/phenyl conjugates and evaluation of their antimicrobial activity

Abstract

Novel xanthene-triazole-quinoline/phenyl conjugates were synthesized by eco-friendly one pot three-component condensation of 12-aryl-2-hydroxy- tetrahydrobenzo[a]xanthene-11- one, propargyl bromide and 4-azido-7- chloroquinoline/phenyl azide using polyethylene glycol (PEG-400) as a reaction medium with an aim to explore their effect on the in vitro growth of microorganisms causing microbial infection. All newly synthesized xanthene-triazole-quinoline/ phenyl conjugates were fully characterized and were evaluated for in vitro antibacterial and antifungal activity. Antimicrobial activity was evaluated against nine microbial strains. All compounds showed good Gram positive antibacterial and antifungal activity. One of the compounds showed best antibacterial and antifungal activity. Further, binding mode of this compound at the active site of enzyme topoisomerase II DNA gyrase B has also been investigated. ©2014 Sociedade Brasileira de Química.