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  • Title: Synthesis and biological evaluation of beta-chloro vinyl chalcones as inhibitors of TNF-alpha and IL-6 with antimicrobial activity.
    Author: Bandgar BP, Patil SA, Korbad BL, Nile SH, Khobragade CN.
    Journal: Eur J Med Chem; 2010 Jun; 45(6):2629-33. PubMed ID: 20171758.
    Abstract:
    A series of beta-chloro vinyl chalcones have been synthesized by Claisen-Schmidt condensation. beta-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-alpha 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 microM concentration. None of the compound was found to be cytotoxic in CCK-8 cells at 10 microM concentration. Whereas compounds 5b, 5d, 5e and 5i showed very good antibacterial activity and compounds 5a, 5b, 5e and 5i showed good antifungal activity.
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