Design, Synthesis and Pharmacological Screening of Novel Flavone Derivatives

Abstract

Sabale Prafulla31961*, Potey Lata31962, Sayyad Nusrat31963 and Rahangdale Priya31964

Flavonoids are the natural phytoconstituents widely distributed in plants originate in fruits, vegetables, grains, bark, roots, stems, flowers, tea and wine. Flavonoids have been recognized as secondary metabolites of plant, with marked biological significance such as Anti-inflammatory, Antioxidant, Anticancer and Antimicrobial activity. Hence, flavonoids are considered as an indispensable component in a variety of nutraceutical, pharmaceutical, medicinal and cosmetic applications with versatile health benefits.

Research on flavonoids received an added impulse with the discovery on Anti-inflammatory by several mechanisms, but the most important mechanism is the inhibition of eicosanoids generating enzyme. In present research a novel series of synthetic flavones (1a-l) have been synthesized after Molecular Docking studies. Synthesis of novel flavones was carried out using 2, 4-dihydroxyacetophenone as starting material through Baker-Venkataraman Reaction and then finally condensed with substituted acyl chloride. All the synthesized compounds was confirmed by their physicochemical properties and spectral studies. Novel flavone derivatives were assessed for anti-inflammatory activity by using Carrageenan induced rat paw edema method. Novel flavone derivatives were performed to establish correlation between biological activity and molecular properties. Among the synthesized compounds (1b, 1g, 1i, 1j 1l) showed good anti-inflammatory activity, whereas compounds (1c, 1e, 1f, 1h, 1k) showed moderate anti-inflammatory activity comparable to the reference drug Indomethacin. Thus, the conclusion can be made that the flavone moiety may exhibit a good anti-inflammatory activity.