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, C. 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

28 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. © 2007 Elsevier Ltd. All rights reserved.

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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