Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists

Research output: Contribution to journalJournal articleResearchpeer-review

  • Ulven, Elisabeth Rexen
  • Maria E Due-Hansen
  • Christian Urban
  • Manuel Grundmann
  • Ralf Schröder
  • Brian D Hudson
  • Graeme Milligan
  • Michael A Cawthorne
  • Evi Kostenis
  • Matthias U Kassack
  • Ulven, Trond
FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Volume55
Issue number14
Pages (from-to)6624-6628
Number of pages5
ISSN0022-2623
DOIs
Publication statusPublished - 2012
Externally publishedYes

ID: 189162178