2634-33-5Relevant articles and documents
Novel palladium(II) and platinum(II) complexes of biocidal benzisothiazolinone (Bit); X-ray crystal structures of co-crystallised Bit/BitO and cis-Pd(en)(Bit-1H)2·H2O
Griffith, Darren M.,Haughey, Aisleen,Chahal, Sunisha,Müller-Bunz, Helge,Marmion, Celine J.
, p. 2333 - 2337 (2010)
Reaction of benzisothiazolinone (Bit), a well-known biocide, with the Pd(II) and Pt(II) am(m)ine precursors cis-[Pd(en)(H2O) 2](NO3)2 and cis-[Pt(NH3) 2(H2O)2](NO
Method for preparing 1, 2-benzisothiazolin-3-one through catalytic oxidation
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Paragraph 0025; 0029, (2021/08/06)
The invention provides a method for preparing 1, 2-benzisothiazoline-3-one through catalytic oxidation, which comprises the following steps of: by taking a metal manganese salt or a manganese complex as a catalyst, carrying out oxidative cyclization react
Synthesis method of 1, 2-benzisothiazoline-3-ketone
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Paragraph 0047-0054, (2021/04/10)
The invention discloses a synthesis method of 1, 2-benzisothiazoline-3-ketone, which comprises the following steps: (1) adding 1, 2-dimercaptoethane and potassium carbonate at room temperature at one time, stirring, and slowly heating to obtain a mercapto
Bioisosteric investigation of ebselen: Synthesis and in vitro characterization of 1,2-benzisothiazol-3(2H)-one derivatives as potent New Delhi metallo-β-lactamase inhibitors
Jin, Wen Bin,Xu, Chen,Cheung, Qipeng,Gao, Wei,Zeng, Ping,Liu, Jun,Chan, Edward W.C.,Leung, Yun-Chung,Chan, Tak Hang,Wong, Kwok-Yin,Chen, Sheng,Chan, Kin-Fai
, (2020/04/30)
Carbapenem-resistant Enterobacteriaceae (CRE) producing New Delhi metallo-β-lactamase (NDM-1) cause untreatable bacterial infections, posing a significant threat to human health. In the present study, by employing the concept of bioisosteric replacement of the selenium moiety of ebselen, we have designed, synthesized and characterized a small compound library of 2-substituted 1,2-benzisothiazol-3(2H)-one derivatives and related compounds for evaluating their cytotoxicity and synergistic activity in combination with meropenem against the E. coli Tg1 (NDM-1) strain. The most promising compound 3a demonstrated potent synergistic activity against a panel of clinically isolated NDM-1 positive CRE strains with FICI as low as 0.09. Moreover, its IC50 value and inhibition mechanism were also confirmed by using the enzyme inhibition assay and the ESI-MS analysis respectively. Importantly, compound 3a has acceptable toxicity and is not a PAINS. Because of its structural simplicity and potent synergistic activity in combination with meropenem, we propose that compound 3a may be a promising meropenem adjuvant and a new series of such compounds may worth further investigations.