1330593-67-3Relevant academic research and scientific papers
Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1)
Chapman, Timothy M.,Osborne, Simon A.,Bouloc, Nathalie,Large, Jonathan M.,Wallace, Claire,Birchall, Kristian,Ansell, Keith H.,Jones, Hayley M.,Taylor, Debra,Clough, Barbara,Green, Judith L.,Holder, Anthony A.
, p. 3064 - 3069 (2013/06/26)
A series of imidazopyridazines which are potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) was identified from a high-throughput screen against the isolated enzyme. Subsequent exploration of the SAR and optimisation has yielded leading members which show promising in vitro anti-parasite activity along with good in vitro ADME and selectivity against human kinases. Initial in vivo testing has revealed good oral bioavailability in a mouse PK study and modest in vivo efficacy in a Plasmodium berghei mouse model of malaria.
