2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: a new class of protein tyrosine phosphatase 1B inhibitors

David R. Adams, Achamma Abraham, Jun Asano, Catherine Breslin, Colin A.J. Dick, Ulrich Ixkes, Blair F. Johnston, Derek Johnston, Justin Kewnay, Simon P. Mackay, Simon J. MacKenzie, Morag McFarlane, Lee Mitchell, Daniel Spinks, Yasuo Takano

Research output: Contribution to journalArticlepeer-review

25 Citations (Scopus)


A new series of non-peptidic, mono-acid protein tyrosine phosphatase 1B (PTP1B) inhibitors has been identified by structure-based design. Compounds with 2-(indol-3-yl)- and 2-phenyl-3,3,3-trifluoro-2-hydroxypropionic acid core units targeted at the enzyme's primary site and a hydrophobic chlorophenylthiazole extension in its 2° site exhibit 3-60 μM IC50s for PTP1B inhibition in an Sf9 cell-based assay.

Original languageEnglish
Pages (from-to)6579-6583
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number23
Publication statusPublished - 1 Dec 2007


  • diabetes
  • indole
  • inhibitor
  • insulin resistance
  • insulin sensitivity
  • obesity
  • phospho-tyrosine
  • protein tyrosine phosphatase 1B
  • PTP1B
  • structure-based design
  • thiazole


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