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, 14 (7), 1655-9

Lactams as EP4 Prostanoid Receptor Subtype Selective Agonists. Part 1: 2-Pyrrolidinones-stereochemical and Lower Side-Chain Optimization

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Lactams as EP4 Prostanoid Receptor Subtype Selective Agonists. Part 1: 2-Pyrrolidinones-stereochemical and Lower Side-Chain Optimization

Todd R Elworthy et al. Bioorg Med Chem Lett.

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 EP(4) 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 EP(4) versus the other EP prostanoid receptors.

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