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Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists

Epple, Robert and Azimioara, Mihai and Alper, Phillip and Cow, Christopher and Mutnick, Daniel and Nikulin, Victor and Lelais, Gerald and Mcneill, Matthew and Michellys, Pierre and Wang, Zhiliang and Li, Jing and Bao, Dingjiu and Zoll, Jocelyn and Kim, Young and Zimmerman, Matthew and Groessl, Todd and Tuntland, Tove and Mcnamara, Peter and Seidel, Martin (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: 22 Nov 2017 00:45
Last Modified: 25 Jan 2019 00:46


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