Synthesis and bioactivity of novel benzisothiazolone derivatives as potential microbiocides

Novel microbiocides 2‐(hydroxymethyl)benzo[ d ]isothiazol‐3(2 H )‐one (7) and (3‐oxobenzo[ d ]isothiazol‐2(3 H )‐yl)methyl benzencarboxylates 11a , 11b , 11c were synthesized in good yields, and their structures were characterized by means of 1 H NMR, MS, and elemental analysis. The new compounds were tested preliminarily in laboratory assays against the aquicolous bacteria including Escherichia coli, Staphyloccus aurueus, Vibrio alginolyticus, Aeromonas hydrophila , and Bacillus subtilis . The results show all the synthesized compounds have good antimicrobial activity . The antimicrobial activity of all the tested compounds against all test bacteria is >96.6% at the concentration of 10 −2 mg mL −1 . These compounds can be further developed for effective microbiocides in the future. J. Heterocyclic Chem., 46 , 320 (2009).