Design and synthesis of potent, non-peptidic inhibitors of HPTPbeta

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4252-6. doi: 10.1016/j.bmcl.2006.05.074. Epub 2006 Jun 12.


The sulfamic acid phosphotyrosine mimetic was coupled with a previously known malonate template to obtain highly selective and potent inhibitors of HPTPbeta. Potentially hydrolyzable malonate ester functionalities were replaced with 1,2,4-oxadiazoles without a significant effect on HPTPbeta potency.

MeSH terms

  • Chemistry, Pharmaceutical / methods*
  • Crystallography, X-Ray
  • Drug Design
  • Hydrogen Bonding
  • Hydrolysis
  • Models, Chemical
  • Models, Molecular
  • Molecular Structure
  • Nerve Tissue Proteins / antagonists & inhibitors*
  • Protein Tyrosine Phosphatases / antagonists & inhibitors*
  • Receptor-Like Protein Tyrosine Phosphatases, Class 5
  • Structure-Activity Relationship


  • Nerve Tissue Proteins
  • Protein Tyrosine Phosphatases
  • Receptor-Like Protein Tyrosine Phosphatases, Class 5