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

ABSTRACT: 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.

SUBMITTER: Tsagris DJ 

PROVIDER: S-EPMC6193536 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature

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

Tsagris Denise J DJ   Birchall Kristian K   Bouloc Nathalie N   Large Jonathan M JM   Merritt Andy A   Smiljanic-Hurley Ela E   Wheldon Mary M   Ansell Keith H KH   Kettleborough Catherine C   Whalley David D   Stewart Lindsay B LB   Bowyer Paul W PW   Baker David A DA   Osborne Simon A SA  

Bioorganic & medicinal chemistry letters 20180827 19

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. ...[more]

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