Sarah Schleiferböck 1 , 2 , Christian Scheurer 1 , 2 , Masataka Ihara 3 , 4 , Isamu Itoh 3 , 4 , Ian Bathurst 5 , Jeremy N Burrows 5 , Pascal Fantauzzi 5 , Julie Lotharius 5 , Susan A Charman 6 , Julia Morizzi 6 , David M Shackleford 6 , Karen L White 6 , Reto Brun 1 , 2 , Sergio Wittlin 1 , 2
15 November 2013
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.