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Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Feb 01; Vol. 19 (3), pp. 675-9. Date of Electronic Publication: 2008 Dec 24. - Publication Year :
- 2009
-
Abstract
- Amino ketone warheads were explored as alternatives to the nitrile group of a potent and selective cathepsin K inhibitor. The resulting compounds were potent and selective inhibitors of cathepsin K and these nitrile replacements had a significant effect on metabolism and pharmacokinetics.
- Subjects :
- Animals
Bile metabolism
Biphenyl Compounds chemistry
Drug Design
Humans
Inhibitory Concentration 50
Ketones analysis
Models, Chemical
Osteoporosis drug therapy
Rats
Structure-Activity Relationship
Time Factors
Biphenyl Compounds chemical synthesis
Cathepsin K antagonists & inhibitors
Cathepsin K chemistry
Chemistry, Pharmaceutical methods
Ketones chemistry
Nitriles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19117756
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.12.053