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Potent inhibitors of malarial P. Falciparum protein kinase G: Improving the cell activity of a series of imidazopyridines
- Source :
- Bioorganic & Medicinal Chemistry Letters
- Publication Year :
- 2019
- Publisher :
- Elsevier BV, 2019.
-
Abstract
- Graphical abstract<br />Development of a class of bicyclic inhibitors of the Plasmodium falciparum cyclic GMP-dependent protein kinase (PfPKG), starting from known compounds with activity against a related parasite PKG orthologue, is reported. Examination of key sub-structural elements led to new compounds with good levels of inhibitory activity against the recombinant kinase and in vitro activity against the parasite. Key examples were shown to possess encouraging in vitro ADME properties, and computational analysis provided valuable insight into the origins of the observed activity profiles.
- Subjects :
- Imidazopyridine
Pyridines
Plasmodium falciparum
Clinical Biochemistry
Protein kinase G
Pharmaceutical Science
Ligands
01 natural sciences
Biochemistry
Article
law.invention
Antimalarials
Structure-Activity Relationship
Parasitic Sensitivity Tests
law
Drug Discovery
Cyclic GMP-Dependent Protein Kinases
Protein kinase A
Protein Kinase Inhibitors
Molecular Biology
ComputingMethodologies_COMPUTERGRAPHICS
ADME
Dose-Response Relationship, Drug
Molecular Structure
biology
010405 organic chemistry
Kinase
Chemistry
Organic Chemistry
Imidazoles
biology.organism_classification
In vitro
Malaria
0104 chemical sciences
3. Good health
010404 medicinal & biomolecular chemistry
Recombinant DNA
Molecular Medicine
cGMP-dependent protein kinase
SAR
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 29
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....a01a5f293ace057b567da68eeb378c47