Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K

The structure-based design and synthesis of lactam-constrained azapeptide inhibitors of human cathepsin K are described. Enhanced stability to proteolytic cleavage over acyclic analogues is discussed. The structure-based design and synthesis of lactam-constrained azapeptide inhibitors (e.g., 2) of h...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-07, Vol.9 (14), p.1907-1910
Hauptverfasser:	Duffy, Kevin J., Ridgers, Lance H., DesJarlais, Renee L., Tomaszek, Thaddeus A., Bossard, Mary J., Thompson, Scott K., Keenan, Richard M., Veber, Daniel F.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amines - chemistry Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cathepsin K Cathepsins - antagonists & inhibitors Cathepsins - metabolism Crystallography, X-Ray Cysteine Proteinase Inhibitors - chemical synthesis Cysteine Proteinase Inhibitors - metabolism Cysteine Proteinase Inhibitors - pharmacology Drug Design Humans Medical sciences Models, Molecular Osteoclasts - enzymology Peptides - chemistry Pharmacology. Drug treatments Pyrrolidinones - chemical synthesis Pyrrolidinones - metabolism Pyrrolidinones - pharmacology Structure-Activity Relationship
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Zusammenfassung:	The structure-based design and synthesis of lactam-constrained azapeptide inhibitors of human cathepsin K are described. Enhanced stability to proteolytic cleavage over acyclic analogues is discussed. The structure-based design and synthesis of lactam-constrained azapeptide inhibitors (e.g., 2) of human osteoclast cathepsin K are described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00322-4