Synthesis, characterization, molecular docking studies and biological activity ofcoumarin linked 2-pyridone heterocycles

Desai, Nisheeth C; Karkar, Tushar J; Vekariya, Rajesh H; Joshi, Surbhi B; Jadeja, Krunalsinh A; Vaja, Darshita V

Abstract

In the present paper, the synthesis, characterization, antimicrobial activity and in silico molecular docking study of6-((arylidene)amino)-4-(4-chlorophenyl)-2-oxo-1-((1-(2-oxo-2H-chromen-3-yl)ethylidene)amino)-1,2-dihydropyridine-3,5-dicarbonitriles 4a-o have been reported. Compounds 4d, 4g, 4j, 4k, 4m and 4o show significant activity. Structuredetermination of the synthesized compounds has been done by the standard spectroscopic techniques. It is observed thatbiological activity is influenced by electronic environment of the molecules. Electron withdrawing group at para positionplays a major role for enhancing the biological activity for antibacterial activity and the electron donating group at paraposition for antifungal activity. Compounds 4a-o have been further evaluated for cytotoxicity on HeLa cells. From thecytotoxicity results, compounds have been found to possess low cytotoxicity with potent antimicrobial activity.


Keyword(s)

Medicinal chemistry, antibacterial, antifungal, cytotoxicity, molecular docking

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