Gallic acid derived diarylpropanones exhibit synergistic antibacterial activities

Development of resistance against most of the clinical antibiotics is a menace to mankind for their use in future. Present study aimed at design and synthesis of some microtubule dynamics modulators as antibacterial and anticancer agents. Eight diverse Aza Michael adducts were prepared at diarylpropenone core possessing desired motifs in 38–57% yields. Compound 6b showed significant antiproliferative activity against K562, leukemic cell line. While compound 6h exhibited potent antibacterial activity against methicillin resistant Staphylococcus aureus and methicillin resistant S. epidermidis. In the checkerboard experiment, 6h showed synergistic effect in combination of penicillin and also with norfloxacin, up to four-fold reduction in quantity of the antibiotic drug. Its effect was bacteriostatic as evident from time kill assay. The 3,4,5-trimethoxyphenyl motif induces antitubulin effect in Aza Michael adduct 6b for anticancer activity. Both the leads can further be optimized for better efficacy in future.