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

Autor:	Nathalie Bouloc, Paul W. Bowyer, Keith H. Ansell, Jonathan M. Large, Kristian Birchall, Catherine A. Kettleborough, Denise J. Tsagris, David A. Baker, Ela Smiljanic-Hurley, Mary C. Wheldon, Lindsay B. Stewart, David Whalley, Simon A. Osborne, Andy Merritt
Rok vydání:	2018
Předmět:	0301 basic medicine Alkylation Plasmodium falciparum Clinical Biochemistry Protozoan Proteins Pharmaceutical Science 01 natural sciences Biochemistry Article Antimalarials Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound parasitic diseases Drug Discovery Cyclic GMP-Dependent Protein Kinases Humans Protein kinase A Thiazole Protein Kinase Inhibitors Molecular Biology ADME chemistry.chemical_classification biology 010405 organic chemistry Kinase Chemistry Organic Chemistry biology.organism_classification In vitro 0104 chemical sciences Thiazoles 030104 developmental biology Enzyme Molecular Medicine Oxidation-Reduction cGMP-dependent protein kinase
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 28:3168-3173
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2018.08.028
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49b91d780c2345c0f96aac2b5f0ee17a https://doi.org/10.1016/j.bmcl.2018.08.028 Zobrazit plný text záznamu Full Text from ScienceDirect