F. Zani et P. Vicini, ANTIMICROBIAL ACTIVITY OF SOME 1,2-BENZISOTHIAZOLES HAVING A BENZENESULFONAMIDE MOIETY, Archiv der pharmazie, 331(6), 1998, pp. 219-223
Some sulfonamide and sulfonylurea derivatives of unsubstituted and 5-m
ethylsubstituted 1,2-benzisothiazole were studied in vitro for their a
ntimicrobial properties against bacteria and fungi. Compounds 7 and 8
exhibited good antibacterial activity against Gram positive bacteria.
A strong synergism was observed when their growth-inhibitory effect wa
s assayed in combination with trimethoprim by using Bacillus subtilis
and Staphylococcus aureus as test microorganisms. The antimycotic acti
on of benzenesulfonylurea derivative 9 was very marked for Madurella m
ycetomatis and dermatophytes Epidermophyton floccosum, Microsporum gyp
seum and Trichophyton spp.. Structure-activity relations are discussed
.