Abstract
A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.
MeSH terms
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Animals
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Antimalarials / chemical synthesis*
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Antimalarials / chemistry
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Antimalarials / pharmacology*
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Combinatorial Chemistry Techniques
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Drug Design
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology*
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Inhibitory Concentration 50
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KB Cells
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Mitogen-Activated Protein Kinase Kinases / antagonists & inhibitors*
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Molecular Structure
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Plasmodium falciparum / drug effects
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Plasmodium falciparum / enzymology*
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Protozoan Proteins / antagonists & inhibitors*
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Pyridazines / chemical synthesis*
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Pyridazines / chemistry
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Pyridazines / pharmacology*
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Structure-Activity Relationship
Substances
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Antimalarials
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Imidazoles
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Protozoan Proteins
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Pyridazines
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PK7 protein, Plasmodium falciparum
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Mitogen-Activated Protein Kinase Kinases