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CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.
CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Dec 20; Vol. 14 (24), pp. 6017-21. - Publication Year :
- 2004
-
Abstract
- New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50=380 nM rat mitochondria) with favorable PK properties (F=93%, t(1/2)=13.6h, dog).
- Subjects :
- Administration, Oral
Animals
Biological Availability
Dogs
Fatty Acids chemistry
Humans
Molecular Conformation
Oxidation-Reduction drug effects
Palmitoyl Coenzyme A metabolism
Rats
Structure-Activity Relationship
Antioxidants pharmacokinetics
Antioxidants pharmacology
Fatty Acids metabolism
Oxadiazoles pharmacokinetics
Oxadiazoles pharmacology
Palmitoyl Coenzyme A antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 14
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15546720
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.09.077