Synthesis and Activity Study of 1,2-Benzisothiazol-3-one Derivatives
1,2-Benzisothiazol-3-one(BIT)exhibits limited antibacterial activity,prompting the search for new antibacterial drugs.In this study,BIT was used as the starting compound to synthesize 17 new N-substituted alkoxymethylbenzoisothia-zolone derivatives through one-pot reaction method involving BIT,aldehyde,and alcohol.The reaction pathways were inves-tigated using density functional theory(DFT),and the inhibitory activity of the new compounds against bacteria,fungi,and crop pathogens was evaluated.The results demonstrated that these compounds displayed strong inhibitory effects on Staphy-lococcus aureus and Candida albicans,with most compounds exhibiting minimum inhibitory concentrations(MIC)ranging from 1 mg/L to 4 mg/L.Compounds BIT-5,BIT-9,BIT-10,and BIT-11 exhibited high inhibitory activity against various bac-teria and fungi tested,particularly against agricultural crop disease fungi such as Sclerotinia sclerotiorum,Fusarium pseudograminearum,Fusarium graminearum,and Gaeumannomyces gramims,with MIC values in the range of 5～10 mg/L,which has further research value.
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