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Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG)

2018; Elsevier BV; Volume: 28; Issue: 19 Linguagem: Inglês

10.1016/j.bmcl.2018.08.028

1464-3405

Denise J. Tsagris, Kristian Birchall, Nathalie Bouloc, Jonathan M. Large, Andy Merritt, Ela Smiljanic-Hurley, Mary C. Wheldon, Keith H. Ansell, Catherine Kettleborough, David Whalley, Lindsay B. Stewart, Paul W. Bowyer, David A. Baker, Simon A. Osborne,

HIV/AIDS drug development and treatment

A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria.