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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. (2013)
Publisher: Elsevier Science Ltd
Journal: Bioorganic & Medicinal Chemistry Letters
Languages: English
Types: Article
Subjects: Molecular Biology, SAR, Pharmaceutical Science, Malaria, Article, Drug Discovery, Organic Chemistry, Plasmodium falciparum, Biochemistry, Molecular Medicine, Imidazopyridazine, Clinical Biochemistry, Calcium-dependent protein kinase 1

Classified by OpenAIRE into

mesheuropmc: parasitic diseases
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.

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  • EC | EVIMALAR

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