Description
BTZ-N3 is a potent and selective anti-TB drug candidate. BTZ-N3 is a related click chemistry products based on the molecular mode of activation of BTZ043. BTZ-N3 binds in the essentially same pocket as that of BTZ043. Detailed biochemical studies with cell envelope enzyme fractions_x000D_
of Mycobacterium smegmatis combined with the model biochemical reactivity studies with nucleophiles indicated that, in contrast to BTZ043, the azide analogue may have a different mode of activation for anti-TB activity. Subsequent enzymatic studies with recombinant DprE1 from Mtb followed by MIC determination in NTB1 strain of Mtb (harboring Cys387Ser mutation in DprE1 and is BTZ043 resistant) unequivocally indicated that BTZ-N3 is an effective reversible and noncovalent inhibitor of DprE1.
Uses
BTZ-N3 is a potent reversible and noncovalent inhibitor of decaprenylphosphoryl-β-d-ribose 2′ oxidase (DprE1) that shows anti-tuberculosis activity[1].
References
[1] Rohit Tiwari, et al. Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043. ACS Med Chem Lett. 2016 Jan 4;7(3):266-70.
