Lactams as EP 4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization

…, MG Roepel, L Quattrocchio-Setti, DB Smith…

文献索引：Elworthy, Todd R; Kertesz, Denis J; Kim, Woongki; Roepel, Michael G; Quattrocchio-Setti, Lina; Smith, David B; Tracy, Jahari Laurant; Chow, Audrey; Li, Fujun; Brill, Emma R; Lach, Leang K; McGee, Daren; Yang, Diana S; Chiou, San-San Bioorganic and medicinal chemistry letters, 2004 , vol. 14, # 7 p. 1655 - 1659

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被引用次数: 18

摘要

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 (eg, 17, 24, 30, 31, and 33) of high potency and greater than 1000-fold affinity for EP4 versus the other EP prostanoid receptors.