NEU-730 is a novel inhibitor of TbrPDEB1, showing modest inhibition of T. brucei proliferation.
Uses
PDEB1-IN-1 (Compound 12b) is the derivative of Cilomilast (HY-10790), and serves as an inhibitor for TryPanosoma Brucei PDEB1 (TbrPDEB1) with an IC50 of 0.95 μM. PDEB1-IN-1 inhibits the proliferation of T. Brucei with an EC50 of 26 μM[1].
References
[1] Amata E, et al., Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4084-9. DOI:10.1016/j.bmcl.2014.07.063
