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Review
. 2019;19(12):999-1014.
doi: 10.2174/1389557518666181015151801.

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

Emiliya V Nosova  1   2 , Galina N Lipunova  1 , Valery N Charushin  1   2 , Oleg N Chupakhin  1   2
Affiliations
Review

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

Emiliya V Nosova et al. Mini Rev Med Chem. 2019.

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

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