Design and Discovery of Some Novel Chalcones as Antioxidant and Anti-Inflammatory Agents via Attenuating NF-κB.

Concerning the role of antioxidant and anti-inflammatory agents for hepatic fibrosis patients, the current study deals with the development of novel chalcone derivatives 5a-i via efficient synthetic methodology in a two-step reaction involving Claisen-Schmidt condensation. The obtained target analogs were screened for in vitro antioxidant activity by various methods (H2 O2 , DPPH, ferrous reducing power, and nitric oxide), where they exhibit considerable radical scavenging activity. These compounds were also evaluated for inhibitory potency against NF-κB activation induced by LPS for the determination of their anti-inflammatory activity. The inhibition values indicate that the entire set of compounds efficiently inhibits the NF-κB activation provoked by LPS. Among the series, compound 5i was identified as the most potent inhibitor of NF-κB, with a relative NF-κB activity of 1.12 ± 0.53. It also inhibits various inflammatory mediators, such as TNF-α, IL-1β, IL-6, and PGE2 .