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Drug Des Devel Ther. 2013 Nov 15;7:1377-84. doi: 10.2147/DDDT.S51298. eCollection 2013.

In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models.

Author information

1
Swiss Tropical and Public Health Institute, Basel, Switzerland ; University of Basel, Basel, Switzerland.

Abstract

The objective of this work was to characterize the in vitro (Plasmodium falciparum) and in vivo (Plasmodium berghei) activity profile of the recently discovered lead compound SSJ-183. The molecule showed in vitro a fast and strong inhibitory effect on growth of all P. falciparum blood stages, with a tendency to a more pronounced stage-specific action on ring forms at low concentrations. Furthermore, the compound appeared to be equally efficacious on drug-resistant and drug-sensitive parasite strains. In vivo, SSJ-183 showed a rapid onset of action, comparable to that seen for the antimalarial drug artesunate. SSJ-183 exhibited a half-life of about 10 hours and no significant differences in absorption or exposure between noninfected and infected mice. SSJ-183 appears to be a promising new lead compound with an attractive antimalarial profile.

KEYWORDS:

Plasmodium falciparum; antimalarial studies; cross-resistance; stage-specificity

PMID:
24255594
PMCID:
PMC3832383
DOI:
10.2147/DDDT.S51298
[Indexed for MEDLINE]
Free PMC Article

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