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Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists

Azimioara, Mihai, Epple, Robert, Alper, Phillip, Cow, Christopher, Mutnick, Daniel, Nikulin, Victor, Lelais, Gerald, Mcneill, Matthew, Michellys, Pierre, Wang, Zhiliang, Li, Jing, Bao, Dingjiu, Zoll, Jocelyn, Kim, Young, Zimmerman, Matthew, Groessl, Todd, Tuntland, Tove, Mcnamara, Peter, Seidel, Martin, Joseph, Sean, Mecom, John, Reding, Esther and Paliotti, Michael (2014) Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists. Bioorganic and Medicinal Chemistry Letters, 24 (23). pp. 5478-5483. ISSN 1464-3405


Systematic SAR optimization of the GPR119 agonist lead 1, derived from an internal HTS campaign, led to compound 29. Compound 29 displays significantly improved in vitro activity and oral exposure, leading to GLP1 elevation in acutely dosed mice and reduced glucose excursion in an OGTT study in rats at doses ≥10 mg/kg.

Item Type: Article
Keywords: GPCR agonists GPR119 Tricyclic pyrazolopyrimidines Type 2 diabetes
Date Deposited: 21 Nov 2017 00:45
Last Modified: 25 Jan 2019 00:46


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