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Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2005 May 16; Vol. 15 (10), pp. 2523-6. - Publication Year :
- 2005
-
Abstract
- 2-Piperidones were prepared bearing heptanoic acid or a thioether heptanoic acid at the 1-position as well as appropriately substituted at the 6-position to mimic the structure of prostaglandins. The stereochemical purity at the 6-position was determined to be 95% ee for an advanced synthetic intermediate. The 2-piperidones were identified as potent agonists at the EP4 prostanoid receptor. They displayed a high affinity (Ki 5-130 nM) at EP4 and subtype selectivity.
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 15
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15863309
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.03.059