Antifungal Screening and Oxidation Behavior of some Microwave Assisted Benzothiazine Drugs

Author(s): Neha Mathur, Biplab Manna, Sonlata Bargotya and Ashok Kasana

Some azole and azine series compounds are ubiquitous components both of physiologically active products and of important pharmaceuticals, among them the 4H-1,4-benzothiazine nucleus, known to chemists as azine, is the parent member of a broad spectrum of nitrogen heterocyclic biochemicals commonly found in nature, some of these are highly effective anti-cancer agent, blocking carcinogenic substance, before they reach their cellular targets and eliminating DNA damage in cell nuclei. It may turn out to be a good tranquilizers, anti-inflammatory, antivirals, antibacterial, antimalarial and anti-fungal. 4H-1,4-benzothiazines are nitrogen and sulphur containing heterocyclic compounds, which are analogous to phenothiazines and possess similar structural specificity the presence of a fold along N-S axis, which is important factor for imparting a wide spectrum of pharmacological and biological activities. The molecule has an –(CH=CH)- group replacing phenylene group -(C6H4)- from the phenothiazines. Structural resemblance to these two compounds and their pharmacological and industrial applications have stimulated our interest to construct microwave induced fused benzothiazines libraries on solid phase to find novel hit compounds towards multiple biological targets and better medicinal agents. During the past decades azine series have been developed via substitution patterns, but their oxidation behavior has not yet very popular. So keeping in mind all the industrial and medicinal applications. Our interest to extend studies of benzothiazines with 30% hydrogen-peroxide in glacial acetic acid to study the oxidation of benzothiazines to their sulphones, with a hope to obtain new compounds for therapeutic testing and better medicinal agents. The purity of the synthesized compounds was checked by thin-layer chromatography. Their biological activities along with the physical studies have been done to continue the new research area.

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