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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.
Affiliation
  • Tsagris DJ; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK. Electronic address: denise.tsagris@lifearc.org.
  • Birchall K; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Bouloc N; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Large JM; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Merritt A; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Smiljanic-Hurley E; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Wheldon M; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Ansell KH; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Kettleborough C; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Whalley D; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
  • Stewart LB; Faculty of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK.
  • Bowyer PW; Faculty of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK.
  • Baker DA; Faculty of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK.
  • Osborne SA; LifeArc, Accelerator Building, Open Innovation Campus, Stevenage SG1 2FX, UK.
Bioorg Med Chem Lett ; 28(19): 3168-3173, 2018 10 15.
Article in En | MEDLINE | ID: mdl-30174152
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.
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Full text: 1 Database: MEDLINE Main subject: Plasmodium falciparum / Thiazoles / Protozoan Proteins / Cyclic GMP-Dependent Protein Kinases / Protein Kinase Inhibitors / Antimalarials Limits: Humans Language: En Year: 2018 Type: Article
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Full text: 1 Database: MEDLINE Main subject: Plasmodium falciparum / Thiazoles / Protozoan Proteins / Cyclic GMP-Dependent Protein Kinases / Protein Kinase Inhibitors / Antimalarials Limits: Humans Language: En Year: 2018 Type: Article