AZ 7371

AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-beta-D-ribose 2'-epimerase (DprE1, IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis. It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM). AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Cay-22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6, IC50 = 4 µM).Formal Name: N-(2-hydroxyethyl)-1-[(6-methoxy-5-methyl-4-pyrimidinyl)methyl]-6-methyl-1H-pyrrolo[3,2-b]pyridine-3-carboxamide. CAS Number: 1494675-86-3. Molecular Formula: C18H21N5O3. Formula Weight: 355.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. lambdamax: 215, 297 nm. SMILES: COC1=C(C)C(CN2C=C(C(NCCO)=O)C3=C2C=C(C)C=N3)=NC=N1. InChi Code: InChI=1S/C18H21N5O3/c1-11-6-15-16(20-7-11)13(17(25)19-4-5-24)8-23(15)9-14-12(2)18(26-3)22-10-21-14/h6-8,10,24H,4-5,9H2,1-3H3,(H,19,25). InChi Key: VDRYGTNDKXIPSK-UHFFFAOYSA-N.