Novel pyridone EP4 agonists featuring allylic alcohol ω-chains. Issue 10 (15th May 2020)

• Record Type: Journal Article
• Authors: Dorich, Stéphane; Cox, Jennifer H.; Burch, Jason D.; Chagnon, Félix; Chen, Bin; Léger, Serge; St-Onge, Miguel; Fader, Lee D.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 10(2020)
• Publication Date: 2020-05-15
• Subjects: Prostaglandin E2 receptor 4 (EP4) -- Agonists -- Pyridone -- Allylic alcohol; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2020.127104
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Novel prostaglandin E2 receptor 4 (EP4 ) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists were shown to be selective over EP1, EP2 and EP3 . Analogs harboring a 4-carboxylic acid phenethyl α-chain displayed improved potency over those containing an n -heptanoic acid chain. Key SAR relationships were also identified.