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

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

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 19 , Issue 12 , 2019

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Graphical Abstract:


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, apoprosis.

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Year: 2019
Published on: 15 October, 2018
Page: [999 - 1014]
Pages: 16
DOI: 10.2174/1389557518666181015151801
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