Novel Furanylarylene Arylsulfonylindolesulfonamides: Synthesis and Their Antibacterial Evaluation

概要

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An array of furanylarylene arylsulfonylindolesulfonamides was synthesized through multi-step synthetic protocols involving bromination, stannylation, Stille cross coupling, reduction, arylsulfonylation, chlorosulfonylation, and condensation reactions. As a preliminary evaluation, these analogs were tested for antibacterial activity against a series of bacterial strains such as Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Klebsiella pneumoniae using a two-fold serial dilution assay. Whereas analogs possessing unsubstitution, bromosubstitution, or methyl substitution on the benzene ring of benzenesulfonyl group were less active/inactive, the methoxy and chloro substituted counterparts were demonstrated to be comparatively more active. A few of them were found to exhibit better activity than the standard, streptomycin against selective organisms.
公益社団法人　日本薬学会の論文