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

[ Vol. 19 , Issue. 12 ]

Author(s):

Emiliya V. Nosova*, Galina N. Lipunova, Valery N. Charushin and Oleg N. Chupakhin   Pages 999 - 1014 ( 16 )

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.

Affiliation:

I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, Ekaterinburg, I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, Ekaterinburg, I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, Ekaterinburg, I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, Ekaterinburg

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