Trisubstituted Thiazoles As Potent And Selective Inhibitors Of Plasmodium Falciparum Protein Kinase G (Pfpkg)

Denise Harding,Simon Osborne,Kristian Birchall,Nathalie Bouloc,Jonathan Large,Andy Merritt,Ela Smiljanic-Hurley,Mary Wheldon,Keith Ansell,Catherine Kettleborough,David Whalley,Paul Bowyer,Lindsay Stewart, David Baker

Bioorganic & Medicinal Chemistry Letters（2016）

Cited 24|Views24

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Abstract

•A series of thiazole compounds inhibit the malarial kinase PfPKG.•SAR development of this series led to compound 23.•23 has a biochemical potency of 2 nM and an in vitro cellular potency of 113 nM.•23 also possesses good in vitro ADME and excellent kinase selectivity.

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Key words

Plasmodium falciparum,Malaria,PfPKG,Thiazole

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