An antimalarial agent
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Artefenomel is an ozonide antimalarial agent.1 It is active against 3D7, Cam3.II, and Cam3.II_rev P. falciparum strains (LC50s = 8.7, 4.4, and 6.1 nM, respectively). Artefenomel reduces the number of trophozoites in P. falciparum-infected isolated human red blood cells (IC50 = 31 nM).2 In vivo, artefenomel (30 mg/kg) is 100% curative in a mouse model of P. berghei infection.3
1.Yang, T., Xie, S.C., Cao, P., et al.Comparison of the exposure time dependence of the activities of synthetic ozonide antimalarials and dihydroartemisinin against K13 wild-type and mutant Plasmodium falciparum strainsAntimicrob. Agents Chemother.60(8)4501-4510(2016) 2.Giannangelo, C., Stingelin, L., Yang, T., et al.Parasite-mediated degradation of synthetic ozonide antimalarials impacts in vitro antimalarial activityAntimicrob. Agents Chemother.62(3)e01566-e01617(2018) 3.Kim, H.S., Hammill, J.T., and Guy, R.K.Seeking the elusive long-acting ozonide: Discovery of artefenomel (OZ439)J. Med. Chem.60(7)2651-2653(2017)
DMNPE-caged ATP diammonium salt
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