Abstract
Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3 optimization and identified highly potent and selective cathepsin K inhibitors 11-20.
MeSH terms
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Cathepsin K
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Cathepsins / antagonists & inhibitors*
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Recombinant Proteins / antagonists & inhibitors
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Structure-Activity Relationship
Substances
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Pyrimidines
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Pyrroles
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Recombinant Proteins
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pyrrolopyrimidine
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Cathepsins
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CTSK protein, human
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Cathepsin K