Synthesis and biological evaluation of β-chloro vinyl chalcones as inhibitors of TNF-α and IL-6 with antimicrobial activity

A series of β-chloro vinyl chalcones have been synthesized by Claisen–Schmidt condensation. β-chloro vinyl aldehyde has been synthesized by the Vilsmayer–Hack formylation reaction. The structures of the newly synthesized compounds were confirmed by 1H NMR, IR and Mass spectral analysis. All the compounds were evaluated for their anti-inflammatory activity (against TNF-α and IL-6) and antimicrobial (antibacterial and antifungal) activity. Compounds 5a, 5d, 5e, 5g and 5i exhibited promising activity against IL-6 with 58–83% inhibition at 10 μM concentration. None of the compound was found to be cytotoxic in CCK-8 cells at 10 μM concentration. Whereas compounds 5b, 5d, 5e and 5i showed very good antibacterial activity and compounds 5a, 5b, 5e and 5i showed good antifungal activity.

A series of β-chloro vinyl chalcones have been synthesized by Claisen–Schmidt condensation. All the compounds were evaluated for their anti-inflammatory activity (against TNF-α and IL-6) and antimicrobial activity.Figure optionsDownload as PowerPoint slide