Synthesis and Biological Activity of 2-Amino- and 2-aryl (Heteryl) Substituted 1,3-Benzothiazin-4-ones

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Author(s): Emiliya Nosova*, Galina Lipunova, Valery Charushin, Oleg Chupakhin.

Journal Name: Mini-Reviews in Medicinal Chemistry

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Tuberculosis (TB) takes the second place among the reasons for mortality from infectious diseases. For this reason, the problem of tuberculosis treatment requires urgent attention all over the world. Some 2-amino substituted 1,3-benzothiazin-4-ones (2-amino-1,3-BTZs) represent a promising new class of antitubercular agents. Other 1,3-benzothiazin-4-one derivatives, mostly 2-aryl and 2- (pyridin-2-yl) ones, are attractive due to their ability to suppress oxidative stress-induced cardiomyocyte apoptosis. This review covers the synthetic approaches to 2-amino- and 2-aryl(heteryl) substituted 1,3-benzothiazin-4-ones (1,3-BTZs). A brief overview of structure-activity relationships is presented.

Keywords: Antitubercular agent, 1, 3-Benzothiazin-4-one, Cyclocondensation, 2-Mercaptobenzoic acid, 2-Halogenobenzoyl isothiocyanate.

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(E-pub Ahead of Print)
DOI: 10.2174/1389557518666181015151801
Price: $95