Browse views: by Year, by Function, by GLF, by Subfunction, by Conference, by Journal

Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists

Azimioara, Mihai and Epple, Robert 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 and Joseph, Sean and Mecom, John and 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

Abstract

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
URI: https://oak.novartis.com/id/eprint/22574

Search

Email Alerts

Register with OAK to receive email alerts for saved searches.