Tuberculosis has proved harmful to the entire history of mankind from past several decades. Among the strategies for the development of new anti-tubercular lead compounds, Benzothiazinone (BTZ) were studied, with highly selective mechanism of action on DprE1 (Decaprenyl phosphoryl-b-D-ribose 2-epimerase) flavoenzyme. DprE1 is a vital enzyme for cell wall synthesis, plays a crucial role in the formation of D-arabinofuranose, a component of lipo-arabinomannan and arabinogalactam. Formation of covalent and non-covalent bond by the interacting ligand with the enzyme causes loss of its catalytic activity which ultimately leads to death of the mycobacterium