BTZ-N3 is a novel, potent, selective, reversible and noncovalent inhibitor of DprE1, also an anti-TB (tuberculosis) agent and 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 bioactive compound studies with cell envelope enzyme fractions of Mycobacterium smegmatis combined with the model bioactive compound 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.

纯度：≥98%

CAS：1839081-05-8