Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).
Denise JTsagris;
KristianBirchall;
NathalieBouloc;
Jonathan MLarge;
AndyMerritt;
ElaSmiljanic-Hurley;
MaryWheldon;
Keith HAnsell;
CatherineKettleborough;
DavidWhalley;
+4 more...
Lindsay BStewart;
Paul WBowyer;
David A Baker 
;
Simon AOsborne;
(2018)
Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).
Bioorganic & medicinal chemistry letters, 28 (19).
pp. 3168-3173.
ISSN 0960-894X
DOI: 10.1016/j.bmcl.2018.08.028
;
Simon AOsborne;
(2018)
Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).
Bioorganic & medicinal chemistry letters, 28 (19).
pp. 3168-3173.
ISSN 0960-894X
DOI: 10.1016/j.bmcl.2018.08.028
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.
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- Available under Creative Commons: NC-ND 3.0
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- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6193536 (OA Location)
- 10.1016/j.bmcl.2018.08.028 (DOI)
- 30174152 (PubMed)