Design, Synthesis, Biological Evaluation and In-silico Docking Studies of Some Novel Imidazolone Derivatives As Potent Antimicrobial Containing Fluorine Agents

Abstract

Imidazolones are potent for their intense antimicrobial and mitigating exercises wherein, an assortment of imidazolone analogs 4-aryl-1-(4-chloro-3-fluorophenyl)-2-phenyl-1H-imidazol-5(4H)-ones (2a-o) and 4-aryl-2-phenyl-1-(4-(trifluoromethyl) phenyl)-1H-imidazol-5(4H)-ones (3a-o) were studied amalgamating them by using oxazolones and various aryl amines. Newly synthesized compounds were screened for in vitro activity towards bacterial as well as fungal pathogenic microscopic organisms. Among the synthesized imidazolone derivatives, compound 2f, 2g, 2i, 3b, 3h, and 3k showed moderate antibacterial action while 2d, 2j, 2m, 2n, 3e, 3g, and 3f furnished earmarked antifungal action. In-silico docking of all structures was performed for fungal and bacterial targets. Out of all novel imidazolones, the compounds 2e, 2o and 3o exhibited superior affinity against fungal target 14α-demethylase when compared with other compounds.

GRAPHICAL ABSTRACT

Keywords:

• Oxazolone
• Imidazolone
• Antimicrobial activity
• Molecular docking