Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369062 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
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 significantly improved in vitro activity and oral exposure, to elevate GLP1 acutely in an in vivo mouse model at a dose of 10 mg/kg.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Phil Alper, Mihai Azimioara, Christopher Cow, Daniel Mutnick, Victor Nikulin, Pierre-Yves Michellys, Zhiliang Wang, Esther Reding, Michael Paliotti, Jing Li, Dingjiu Bao, Jocelyn Zoll, Young Kim, Matthew Zimmerman, Todd Groessel, Tove Tuntland,