1247019-14-2Relevant academic research and scientific papers
Benzothiazinones: Prodrugs that covalently modify the decaprenylphosphoryl- β-D-ribose 2′-epimerase DprE1 of mycobacterium tuberculosis
Trefzer, Claudia,Rengifo-Gonzalez, Monica,Hinner, Marlon J.,Schneider, Patricia,Makarov, Vadim,Cole, Stewart T.,Johnsson, Kai
supporting information; experimental part, p. 13663 - 13665 (2010/12/18)
Benzothiazinones (BTZs) form a new class of potent antimycobacterial agents. Although the target of BTZs has been identified as decaprenylphosphoryl- β-d-ribose 2′-epimerase (DprE1), their detailed mechanism of action remains obscure. Here we demonstrate that BTZs are activated in the bacterium by reduction of an essential nitro group to a nitroso derivative, which then specifically reacts with a cysteine residue in the active site of DprE1.
