Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

  • 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.
OriginalsprogEngelsk
TidsskriftJournal of Medicinal Chemistry
Vol/bind55
Udgave nummer14
Sider (fra-til)6624-6628
Antal sider5
ISSN0022-2623
DOI
StatusUdgivet - 2012
Eksternt udgivetJa

ID: 189162178