4.7 Article

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 6, Pages 2629-2633

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.01.050

Keywords

beta-Chloro vinyl chalcones; Anti-inflammatory activity; TNF-alpha; IL-6; Antibacterial activity; Antifungal activity

Funding

  1. Council of Scientific and Industrial Research (CSIR) [01(2023)/05/EMR-II]

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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 H-1 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 mu M concentration None of the compound was found to be cytotoxic in CCK-8 cells at 10 mu M concentration. Whereas compounds 5b, 5d, Se and 5i showed very good antibacterial activity and compounds 5a, 5b, Se and 5i showed good antifungal activity.

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