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The benzo[<i>b</i>]thiophene nucleus and the acylhydrazone functional group were combined to prepare three new series of compounds for screening against <i>Staphylococcus aureus</i>. The reaction of substituted benzo[<i>b</i>]thiophene-2-carboxylic hydrazide and various aromatic or heteroaromatic aldehydes led to a collection of 26 final products with extensive structural diversification on the aromatic ring and on position 6 of the benzo[<i>b</i>]thiophene nucleus. The screening lead to the identification of eight hits, including (<i>E</i>)-6-chloro-<i>N</i>’-(pyridin-2-ylmethylene)benzo[<i>b</i>]thiophene-2-carbohydrazide (<b>II.b</b>), a non-cytotoxic derivative showing a minimal inhibitory concentration of 4 µg/mL on three <i>S. aureus</i> strains, among which were a reference classical strain and two clinically isolated strains resistant to methicillin and daptomycin, respectively.