Novel pyridone EP 4 agonists featuring allylic alcohol ω-chains

Novel prostaglandin E2 receptor 4 (EP ) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists were shown to be selective over EP , EP and EP . Analogs harboring a 4-carboxylic acid phenethyl α-chain displayed improved potency over those containing an n-hep...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2020-05, Vol.30 (10), p.127104
Hauptverfasser:	Dorich, Stéphane, Cox, Jennifer H, Burch, Jason D, Chagnon, Félix, Chen, Bin, Léger, Serge, St-Onge, Miguel, Fader, Lee D
Format:	Artikel
Sprache:	eng
Schlagworte:	Humans Propanols - chemistry Propanols - metabolism Protein Isoforms - agonists Protein Isoforms - metabolism Pyridones - chemistry Pyridones - metabolism Receptors, Prostaglandin E, EP4 Subtype - agonists Receptors, Prostaglandin E, EP4 Subtype - metabolism Structure-Activity Relationship
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Zusammenfassung:	Novel prostaglandin E2 receptor 4 (EP ) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists were shown to be selective over EP , EP and EP . 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.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2020.127104