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Lactams as EP4 prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-stereochemical and lower side-chain optimization.
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.
Affiliation
  • Elworthy TR; Roche Palo Alto, Department of Medicinal Chemistry, 3431Hillview Avenue, Palo Alto, CA 94304-1397, USA. todd.elworthy@roche.com
Bioorg Med Chem Lett ; 14(7): 1655-9, 2004 Apr 05.
Article in En | MEDLINE | ID: mdl-15026044
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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Collection: 01-internacional Database: MEDLINE Main subject: Pyrrolidinones / Receptors, Prostaglandin E / Lactams Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2004 Document type: Article Affiliation country: United States
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Collection: 01-internacional Database: MEDLINE Main subject: Pyrrolidinones / Receptors, Prostaglandin E / Lactams Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2004 Document type: Article Affiliation country: United States