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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 [Bioorg Med Chem Lett] 2019 Feb 01; Vol. 29 (3), pp. 509-514. Date of Electronic Publication: 2018 Nov 20. - Publication Year :
- 2019
-
Abstract
- 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.<br /> (Copyright © 2018 The Authors. Published by Elsevier Ltd.. All rights reserved.)
- Subjects :
- Antimalarials chemical synthesis
Antimalarials chemistry
Cyclic GMP-Dependent Protein Kinases metabolism
Dose-Response Relationship, Drug
Imidazoles chemical synthesis
Imidazoles chemistry
Ligands
Molecular Structure
Parasitic Sensitivity Tests
Plasmodium falciparum enzymology
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Pyridines chemical synthesis
Pyridines chemistry
Structure-Activity Relationship
Antimalarials pharmacology
Cyclic GMP-Dependent Protein Kinases antagonists & inhibitors
Imidazoles pharmacology
Plasmodium falciparum drug effects
Protein Kinase Inhibitors pharmacology
Pyridines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 29
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 30553738
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.11.039