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Novel benzoxazole inhibitors of mPGES-1.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Feb 01; Vol. 23 (3), pp. 907-11. Date of Electronic Publication: 2012 Oct 16. - Publication Year :
- 2013
-
Abstract
- A novel series of potent benzoxazole mPGES-1 inhibitors has been derived from a hit from a high throughput screen. Compound 37 displays mPGES-1 inhibition in an enzyme assay (0.018 μM) and PGE-2 inhibition in a cell-based assay (0.034 μM). It demonstrates 500- and 2500-fold selectivity for mPGES-1 over COX-2 and 6-keto PGF-1α, respectively. In vivo PK studies in dogs demonstrate 55% oral bioavailability and an 7 h half-life.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Amides chemical synthesis
Amides chemistry
Amides pharmacology
Animals
Benzoxazoles chemical synthesis
Benzoxazoles pharmacokinetics
Benzoxazoles pharmacology
Biological Availability
Dogs
Enzyme Activation drug effects
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Humans
Inhibitory Concentration 50
Molecular Structure
Prostaglandin-E Synthases
Structure-Activity Relationship
Benzoxazoles chemistry
Enzyme Inhibitors chemistry
Intramolecular Oxidoreductases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 23
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 23266122
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.10.040