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Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Mar 15; Vol. 16 (6), pp. 1735-9. Date of Electronic Publication: 2006 Jan 11. - Publication Year :
- 2006
-
Abstract
- Starting from a potent pantolactone ketoamide cathepsin K inhibitor discovered from structural screening, conversion of the lactone scaffold to a pyrrolidine scaffold allowed exploration of the S(3) subsite of cathepsin K. Manipulation of P3 and P1' groups afforded potent inhibitors with drug-like properties.
- Subjects :
- Binding Sites
Cathepsin K
Cathepsins chemistry
Crystallography, X-Ray
Humans
Inhibitory Concentration 50
Models, Molecular
Molecular Structure
Serine Proteinase Inhibitors
Structure-Activity Relationship
Amides chemical synthesis
Amides pharmacokinetics
Amides pharmacology
Cathepsins antagonists & inhibitors
Cysteine Proteinase Inhibitors chemical synthesis
Cysteine Proteinase Inhibitors pharmacokinetics
Cysteine Proteinase Inhibitors pharmacology
Ketones chemical synthesis
Ketones pharmacokinetics
Ketones pharmacology
Pyrrolidines chemical synthesis
Pyrrolidines pharmacokinetics
Pyrrolidines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16376075
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.11.101