2012•Journal of Chemical ResearchRequires access

Synthesis and Biological Evaluation of New Thiosubstituted Oxadiazole Derivatives of Coumarin under Solvent-Free Conditionss

Vivek D. Bobade, Sachin V. Patil, Nitin D. Gaikwad

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Abstract

A series of new thiosubstituted 1,3,4-oxadiazole derivatives of coumarin were synthesised by reaction of 7-((5-mercapto-1,3,4-oxadiazol-2-yl)methoxy)-4-methyl-2H-chromen-2-one and α-haloketones by grinding, in solvent-free conditions at room temperature. The reaction was also carried out in ethanol in reflux conditions. Shorter reaction time and better yields were observed in solvent-free conditions. The structures of the compounds were characterised by IR, NMR, elemental analysis and mass spectral data. The synthesised compounds were evaluated for their in vitro antimicrobial screening on different strains of bacteria and fungi. Most of the compounds showed good to moderate activities.

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A series of new thiosubstituted 1,3,4-oxadiazole derivatives of coumarin were synthesised by reaction of 7-((5-mercapto-1,3,4-oxadiazol-2-yl)methoxy)-4-methyl-2H-chromen-2-one and α-haloketones by grinding, in solvent-free conditions at room temperature. The reaction was also carried out in ethanol in reflux conditions. Shorter reaction time and better yields were observed in solvent-free conditions. The structures of the compounds were characterised by IR, NMR, elemental analysis and mass spectral data. The synthesised compounds were evaluated for their in vitro antimicrobial screening on different strains of bacteria and fungi. Most of the compounds showed good to moderate activities.

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Available abstract

A series of new thiosubstituted 1,3,4-oxadiazole derivatives of coumarin were synthesised by reaction of 7-((5-mercapto-1,3,4-oxadiazol-2-yl)methoxy)-4-methyl-2H-chromen-2-one and α-haloketones by grinding, in solvent-free conditions at room temperature. The reaction was also carried out in ethanol in reflux conditions. Shorter reaction time and better yields were observed in solvent-free conditions. The structures of the compounds were characterised by IR, NMR, elemental analysis and mass spectral data. The synthesised compounds were evaluated for their in vitro antimicrobial screening on different strains of bacteria and fungi. Most of the compounds showed good to moderate activities.

Key concepts: Coumarin, Chemistry, Solvent, Oxadiazole, Proton NMR, Ethanol, Organic chemistry, Antimicrobial

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Synthesis and Biological Evaluation of New Thiosubstituted Oxadiazole Derivatives of Coumarin under Solvent-Free Conditionss — Research Paper | ScholarLens