Abstract
In the present study, we successfully synthesized a series of 4-hydroxycoumarin with a variety of aromatic aldehydes via a one-pot route. The excellent results of this-(4-hydroxycoumarin-3yl) methane derivatives were obtained in the presence of 5.0 mol % DMAP as a catalyst in Ethanol at room temperature using conventional and ultrasonication methodologies. All the synthesized compounds were bioactive. The synthesized bis-coumarin derivatives were evaluated for the antibacterial activity (in-vitro) against the Staphylococcus aureus, and the results were compared with the standard Kanamycin. Molecular docking analysis was revealed that compound 3,3'-((2-chlorophenyl)methylene) bis (4-hydroxy-2H-chromen-2-one (3c) showed good interaction with bacterial cystathionine gamma-lyase MccB of Staphylococcus aureus protein (-6.8 kcal/mol binding free energy). The results confirmed that majority of the as-synthesized compounds revealed splendid antibacterial activity. The compound 3c (Minimum inhibitory concentration, 40 μg/mL) shows comparable activity in standard with Kanamycin at the same concentrations against Staphylococcus aureus.
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