Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation

Transcription factor NF-κB and relevant cytokines IL-6 and IL-8 play a pivotal role in thepathogenesis of inflammation. Sinapic acid is a natural product and was demonstrated to possessanti-inflammatory activity. In this paper, we synthesized a series of sinapic acid derivativesand evaluated their anti-inflammatory effects. The result suggested that all of the targetscompounds 7a-j inhibit NF-κB activation and decrease IL-6 and IL-8 expression in BEAS-2B cells. By our biological assays, we found that all of the prepared compounds displayedstronger anti-inflammatory activities than their precursor sinapic acid. Especially, compounds7g and 7i, with electron-drawing groups (nitro and fluoro moieties) in the benzimidazole ring,exhibited remarkable anti-inflammation activity, which was even stronger than the referencedrug dexamethasone.