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

Design, Synthesis, Biological Evaluation and In-silico Docking Studies of Some Novel Imidazolone... 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. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Analytical Chemistry Letters Taylor & Francis

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

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

Abstract

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...
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Publisher
Taylor & Francis
Copyright
© 2021 Har Krishan Bhalla & Sons
ISSN
2230-7532
eISSN
2229-7928
DOI
10.1080/22297928.2021.1944310
Publisher site
See Article on Publisher Site

Abstract

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.

Journal

Analytical Chemistry Letters – Taylor & Francis

Published: Jul 4, 2021

Keywords: Oxazolone; Imidazolone; Antimicrobial activity; Molecular docking

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