Peer-reviewed veterinary case report
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2005
- Authors:
- Barrett, David G et al.
- Affiliation:
- Department of Medicinal Chemistry · United States
- Species:
- rodent
Abstract
An orally bioavailable series of ketoamide-based cathepsin K inhibitors with good pharmacokinetic properties has been identified. Starting from a potent inhibitor endowed with poor drug properties, conformational constraint of the P(2)-P(3) linker and modifications to P(1') elements led to an enhancement in potency, solubility, clearance, and bioavailability. These optimized inhibitors attenuated bone resorption in a rat TPTX hypocalcemic bone resorption model.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/15982880/