The Synthesis And Antibacterial Of Benzisothiazolones

As a class of antimicrobial agents against bacteria and fungi, isothiazolone derivatives have many advantages such as highly efficient, low poisonous, environmentally-friendly and so on. So it has been developed widely and used in medicine, pesticides and industrial fields. In addition such compounds have good activity to kill algae, which makes it be developed as a new type of green marine atifouling agents. The development, function mechanism and biological activity of isothiazolone derivatives are reviewed in this paper.According to the principle of combination of bioactive sub-structure, more than twenty benzisothiazolone derivatives were designed and in which twenty one have never been reported by now. And all the structures were confirmed by means of IR, elemental analysis and ~1H NMR. The optimization to the process of synthesis and the method has been carried on. Their structures are shown as following:(1) Compounds of 3-oxo-N-phenylbenzo[d]isothiazole-2(3H)-carboxamide(2) Compounds of 3-oxobenzo[d]isothiazole-2(3H)-carboxylateThe results of biological activity test showed that most of the compounds synthesized had good inhibitory activity to the growth of tested strains. All the three series of compounds synthesized showed excellent inhibitory activity and even completely inhibited the growth of Bacillus subtilis, Staphylococcus aureus, Blastomyces albicans and Botryodiplodia theobromae.