Synthesis, Antimicrobial Evaluation, and Docking Studies of Substituted New Chromone Linked 1,2,3-Triazoles

ABSTRACT:

In Search of new antibacterial, antifungal agents with improved potency, herein we report the synthesis of a series of new substituted 2-(4-fluorophenyl)-3-((1-phenyl-1H-1,2,3-triazol-4-yl)methoxy)-4H-chromen-4-one derivatives (6a‐q), starting from acetophenone. All the synthesized compounds have been screened for in vitro antibacterial and antifungal activity by using the agar well diffusion method. Among fifteen synthesized compounds, four chromone derivatives i.e. (6a-b), (6h), and (6i) have shown proficient antimicrobial activities. Compound (6a) showed powerful inhibitory activity against all bacterial pathogens but it was not that effective against fungal pathogens on the other hand compound (6b) showed satisfactory activity against fungal pathogens as well. The activity of compounds (6h) and (6i) against S. aureus was remarkable. Other compounds were found active against a few pathogens but activity was good. The compound (6b) was found very effective in inhibiting the growth of S. aureus ATCC 6538 at a low concentration with MIC 190 µg/ml.

Graphical abstract

Keywords:

• 123-Triazoles
• chromones
• antibacterial
• antifungal

Acknowledgments

The author A.S.N. is very grateful to the Head of the Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, for providing the necessary laboratory facilities to carry out the work. We are also thankful to Dr. Babasaheb Ambedkar Marathwada University Sub-campus, Osmanabad for providing biological activity. We are also thankful to SAIF, CSIR-CDRI, Lucknow, and BITS-Pilani, India. For providing spectral analysis data.

Disclosure statement

No potential conflict of interest was reported by the author(s).