Discovery of structurally novel, potent and orally efficacious GPR119 agonists

Screening hit 5 was identified in a biochemical screen for GPR119 agonists. Compound 5 was structurally novel, displayed modest biochemical activity and no oral exposure, but was structurally distinct from typical GPR119 agonist scaffolds. Systematic optimization led to compound 36 with significantl...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-05, Vol.24 (10), p.2383-2387
Hauptverfasser:	Alper, Phil, Azimioara, Mihai, Cow, Christopher, Mutnick, Daniel, Nikulin, Victor, Michellys, Pierre-Yves, Wang, Zhiliang, Reding, Esther, Paliotti, Michael, Li, Jing, Bao, Dingjiu, Zoll, Jocelyn, Kim, Young, Zimmerman, Matthew, Groessel, Todd, Tuntland, Tove, Joseph, Sean B., McNamara, Peter, Seidel, H. Martin, Epple, Robert
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Diabetes Mellitus, Type 2 - drug therapy GPCR agonists GPR119 Humans Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Mice Mice, Inbred C57BL Pyrazoles - chemistry Pyrazoles - pharmacology Pyrazolopyrimidines Pyrimidines - chemistry Pyrimidines - pharmacology Receptors, G-Protein-Coupled - agonists Structure-Activity Relationship Type 2 diabetes
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