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Synthesis and Evaluation of Novel Furfurylidene Derivatives of 2, 6-Diphenyl Piperidin-4-one as Antifungal Agents

Riyaz Ali Osmani, Rahul L. Jadhav, Chandrakant S. Magdum, Rohit R. Bhosale, BhargavR. Harkare, and Prasanna P. Ghodake

The antifungal activity of α, β-unsaturated carbonyl compounds has been recognized generally due to their ability to react with sulfhydryl containing system of fungi essential for normal metabolism.In view of this, number of enones and related compounds were synthesized and evaluated for the antifungal properties. In the present investigation, a series of some novel furfurylidene derivatives of 2,6- diphenyl piperidin-4-one have been synthesized. All compounds were prepared by Claisen-Schmidt condensation between piperidin- 4-one derivatives and furfuraldehyde in the basic medium; led to formation of furfurylidene derivatives. N-aryl sulphonyl and benzoyl derivatives were prepared by reacting furfurylidene piperidin-4-one with aryl sulphonyl chloride and benzoyl chloride. The newly synthesized compounds were found to havepractical yield in range of 68-96% with high purity and their characterization was done using M.P., TLC, FTIR and 1HNMR spectral analysis.All these newly synthesized compounds were then evaluated for their in-vitro antifungal activity against Candida albicans and Aspergillus niger fungal strains in which most of the compounds showed potent activity. The present results may be used as key step for the construction of novel chemical entities with better pharmacological profiles than standard drugs.