1513879-19-0

KDU691 is an antimalarial compound. It inhibits recombinant P. vivax phosphatidylinositol 4-kinase (PI4K) with an IC₅₀ value of 1.5 nM. KDU691 is selective for P. vivax PI4K over recombinant human PI4KβIII and PI3Kα, -β, -γ, and -δ (IC₅₀s = 7.9, 8.8, 2.4, 8, and 3.4 μM, respectively), as well as VPS34 (IC₅₀ = >9.7 μM) and 36 additional kinases in a panel of lipid and protein kinases (IC₅₀s = >10 μM). It is active against P. falciparum and P. yoelii schizonts (IC₅₀s = 0.06 and 0.04 μM, respectively), as well as P. cynomolgi schizonts and hypnozoites (IC₅₀s = 0.11 and 0.2 μM, respectively). KDU691 completely prevents, but does not eradicate established, P. cynomolgi infection in rhesus monkeys when administered at a dose of 20 mg/kg.

KDU691, is a PI4K inhibitor.

Plasmodium

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[1] CASE W. MCNAMARA. Targeting Plasmodium PI(4)K to eliminate malaria[J]. Nature, 2013, 504 7479: 248-253. DOI: 10.1038/nature12782
[2] BIN ZOU*. Lead Optimization of Imidazopyrazines: A New Class of Antimalarial with Activity on Plasmodium Liver Stages[J]. ACS Medicinal Chemistry Letters, 2014, 5 8: 947-950. DOI: 10.1021/ml500244m
[3] A. ZEEMAN. PI4 Kinase Is a Prophylactic but Not Radical Curative Target in Plasmodium vivax-Type Malaria Parasites[J]. Antimicrobial Agents and Chemotherapy, 2016, 60 1: 2858-2863. DOI: 10.1128/aac.03080-15