Title of article
Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization
Author/Authors
Todd R. Elworthy، نويسنده , , Denis J. Kertesz، نويسنده , , Woongki Kim، نويسنده , , Michael G. Roepel، نويسنده , , Lina Quattrocchio-Setti، نويسنده , , David B. Smith ، نويسنده , , Jahari Laurant Tracy، نويسنده , , Audrey Chow، نويسنده , , Fujun Li، نويسنده , , Emma R. Brill، نويسنده , , Leang K. Lach، نويسنده , , Daren McGee، نويسنده , , Diana S. Yang، نويسنده , , San-San Chiou، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
1655
To page
1659
Abstract
A series of 7-[(5R)-substituted 2-oxo-1-pyrrolidinyl]-heptanoic acids were prepared, their isomeric purity determined, and pharmacologically evaluated. Lactams with affinity for the EP4 receptor displayed agonist behavior. The lower side-chain of the lactam template could be substituted to afford ligands (e.g., 17, 24, 30, 31, and 33) of high potency and greater than 1000-fold affinity for EP4 versus the other EP prostanoid receptors.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794254
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