Alper, Phillip and Epple, Robert (2014) Discovery of structurally novel, potent and orally efficacious GPR119 agonists. Bioorganic and Medicinal Chemistry Letters, 24 (10). pp. 2383-2387. ISSN 1464-3405

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. © 2014 Elsevier Ltd. All rights reserved.

Item Type:	Article
Keywords:	GPCR agonists GPR119 Pyrazolopyrimidines Type 2 diabetes
Date Deposited:	14 Mar 2018 00:45
Last Modified:	25 Jan 2019 00:46
URI:	https://oak.novartis.com/id/eprint/11041