616196-46-4Relevant academic research and scientific papers
Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG)
Tsagris, Denise J.,Birchall, Kristian,Bouloc, Nathalie,Large, Jonathan M.,Merritt, Andy,Smiljanic-Hurley, Ela,Wheldon, Mary,Ansell, Keith H.,Kettleborough, Catherine,Whalley, David,Stewart, Lindsay B.,Bowyer, Paul W.,Baker, David A.,Osborne, Simon A.
, p. 3168 - 3173 (2018)
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.
