New hydronaphthalene-sulfonamide derivatives: Synthesis, antimicrobial evaluation and QSAR study.

• A new set of hydronaphthalene-sulfonamides were synthesized in a facile approach. • Some of the synthesized agents reveal potent antimicrobial properties. • The promising candidates showed high level of safety towards the human normal cells. • 2D-QSAR model described the antimicrobial properties observed. In the present work, authors successfully prepared potent antimicrobial agents of new tetrahydronaphthalene-sulfonamide derivatives, derived from new easily synthetic route of 3-methoxy-8-oxo-5,6,7,8-tetrahydronaphthalene-2-sulfonyl chloride 2. Preparation method of this compound has not been published yet, however it is available commercially expensively, which motivated us to innovate new efficient and facile method for its preparation. All the synthesized compounds were tested for in vitro antimicrobial inhibitory activities against a panel of Gram-positive, Gram-negative bacterial pathological strains and Candida Albicans. Compound 2 showed poor activity towards all of the tested pathogenic strains, but it is easily modified and converted from biologically inactive compound to highly active sulfonamide products 5a-f , or moderately active compounds 3a-k. Cytotoxic evaluation of the promising candidates 5d and 5e showed marked safety profile towards the human normal cells. QSAR study for the new compounds was carried out and was compatible with the antimicrobial results. [Display omitted] [ABSTRACT FROM AUTHOR]