Title of article
Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists
Author/Authors
Todd R. Elworthy، نويسنده , , Emma R. Brill، نويسنده , , Christopher C. Caires، نويسنده , , Woongki Kim، نويسنده , , Leang K. Lach، نويسنده , , Jahari Laurant Tracy، نويسنده , , San-San Chiou، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
2523
To page
2526
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.
Keywords
?-Lactams as prostanoids , Selective EP4 ligands , 2-Piperidone , EP4 agonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795619
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