KAR425 is a bipyrrole tambjamines with antimalarial activity against multidrug-resistant P. yoelii in mice.
Uses
KAR425 is a potent and orally active antimalarial agent. KAR425 shows antimalarial activity against the Chloroquine-sensitive (CQS) D6, the Chloroquine-resistant (CQR) Dd2, and 7G8 strains of Plasmodium falciparum, with IC50 values of 62 nM, 55 nM, and 60 nM, respectively[1].
in vivo
KAR425 (25-50 mg/kg/day; Oral gavage; once daily; for 4 days) provides 100% protection to malaria-infected mice until day 28[1].
Animal Model:
4- to 5-week-old female CF1 mice were infected intravenously with P. yoelii[1].
Dosage:
25 and 50 mg/kg/day
Administration:
Oral gavage; once daily; for four successive days
Result:
Provided parasite-free cures on day 28 (100% protection to malaria-infected mice) at 25 and 50 mg/kg/day.
References
[1] Papireddy Kancharla, et al. Synthesis and Structure-Activity Relationships of Tambjamines and B-Ring Functionalized Prodiginines as Potent Antimalarials. J Med Chem. 2015 Sep 24;58(18):7286-309. DOI:10.1021/acs.jmedchem.5b00560
