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CWHM-1552 is an orally efficacious inhibitor of P. falciparum with IC50s of 51 nM and 53 nM for 3D7 and Dd2 strain, respectively[1].
IC50: 51 nM (3D7 strain) and 53 nM (Dd2 strain)[1] CWHM-1552 (Compound (-)-32a) (orally; 3-30 mg/kg/day for 4 days) inhibits parasitemia at 99.9% at 30 mg/kg/day and 94% at 10 mg/kg/day[1]. CWHM-1552 (i.v. administration; 2 mg/kg/day for 48 hours) has respectable half-lives (2.7 h) and low clearance in mice[1]. CWHM-1552 has good pharmacokinetic properties and oral efficacy in a mouse model of malaria. CWHM-1552 has an in vivo ED90 of P. chabaudi ASS infected Mice[1] | [References]
[1]. Meyers MJ, et al. 4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl-N-(4-arylpyrrolidin-3-yl) acetamides. ACS Med Chem Lett. 2019 May, 10(6):966-971. |
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