Synthesis and Biological Evaluation of Benzo[]thiophene Acylhydrazones as Antimicrobial Agents against Multidrug-Resistant .

The benzo[]thiophene nucleus and the acylhydrazone functional group were combined to prepare three new series of compounds for screening against . The reaction of substituted benzo[]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[]thiophene nucleus. The screening lead to the identification of eight hits, including ()-6-chloro-'-(pyridin-2-ylmethylene)benzo[]thiophene-2-carbohydrazide (), a non-cytotoxic derivative showing a minimal inhibitory concentration of 4 µg/mL on three strains, among which were a reference classical strain and two clinically isolated strains resistant to methicillin and daptomycin, respectively.