Abstract
An efficient halogen free ionic liquid (HFIL) N-methyl-2-pyrrolidonium methane sulfonate [HNMP]+[CH3SO3]- catalyzed Biginelli reaction is reported to synthesize naphthoquinone fused dihydropyrimidin-(1H)-ones (DHPM’s). Diversifying this naphthoquinone constituent provides an access to new and interesting DHPM’s for pharmacological profiling. A series of bifunctionalized naphthoquinone-dihydropyrimidin-(1H)-one conjugates (4a-4l) were synthesized and evaluated for their antimicrobial potential against selected bacterial and fungal pathogenic strains. The resulting naphthoquinone fused dihydropyrimidin-(1H)-one hybrids showed significant activities against all the tested Gram positive (Staphylococcus aureus, Bacillus subtilis) and Gram negative (Escherichia coli, Pseudomonas aeruginosa) bacterial pathogens and fungal strains of Aspergillus niger and Aspergillus flavus. Among the series, the DHPM conjugate 4k>4j>4e>4h samples exhibited highest activities against all the tested strains that proved to be important candidates in the drug development against various life threatening diseases. Presently, one-pot, three-component methodology have been developed for the synthesis of bifunctionalized naphthoquinone linked dihydropyrimidin-(1H)-one are being explored for bio-active asymmetric Biginelli scaffolds.
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