AZ 7371

AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC₅₀ = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.¹ 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).² 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 (Item No. 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).

WARNING This product is not for human or veterinary use.

1. Chatterji, M., Shandil, R., Manjunatha, M.R., et al. 1,4-azaindole, a potential drug candidate for treatment of tuberculosis. Antimicrob. Agents Chemother. 58(9), 5325-5331 (2014).

2. Shirude, P.S., Shandil, R., Sadler, C., et al. Azaindoles: Noncovalent DprE1 inhibitors from scaffold morphing efforts, kill Mycobacterium tuberculosis and are efficacious in vivo. J. Med. Chem. 56(23), 9701-9708 (2013).