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Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: Optimization of in vitro activity

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
20
Issue
18
Identifiers
DOI: 10.1016/j.bmcl.2010.07.108
Keywords
  • Flushing
  • Gpr109A
  • Gpr109B
  • Gpcr
  • Lead Identification
  • Lipolysis
  • Niacin
  • Pyrido Pyrimidinone

Abstract

Graphical abstract Pyrido pyrimidinones are selective agonists of the human high affinity niacin receptor GPR109A (HM74A). They show no activity on the highly homologous low affinity receptor GPR109B (HM74). Starting from a high throughput screening hit the in vitro activity of the pyrido pyrimidinones was significantly improved providing lead compounds suitable for further optimization.

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