Butanedioic acid, compd. with 6-fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]-4-quinolinecarboxamide (1:1)

Description

DDD107498 succinate (DDD-498 succinate) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. DDD107498 succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2[1]. EC50: 1 nM (3D7 parasites), 2 nM (WT-PfeEF2)[1]

DDD107498 exhibits an ED90 of 0.57 mg/kg after a single oral dose in mice infected with the rodent parasite P. berghei[1].

References

[1]. BaragaÑa B, et al. A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature. 2015 Jun 18;522(7556):315-20.