Chiral arylpyrrolidinols: preparation and biological profile

Bioorg Med Chem. 2005 May 2;13(9):3117-26. doi: 10.1016/j.bmc.2005.02.054.

Abstract

The preparation and biological evaluation of a new class of arylpyrrolidinols is reported. The antinociceptive activity was evaluated in vivo with the hot plate test (HPT) and formalin test (FT), excluding any involvement on motor coordination with the rota-rod test (RRT). The nociceptive behavior in the late phase of FT (representative of chronic pain) suggests an involvement of the antiinflammatory process and it is clearly influenced by the stereochemical features, being the eutomer of phenylpyrrolidinols, the (2R,3S) enantiomer. Despite this, a specific mechanism of action is not yet clarified.

Publication types

  • Comparative Study

MeSH terms

  • Analgesics / chemical synthesis*
  • Analgesics / chemistry
  • Analgesics / therapeutic use*
  • Animals
  • Crystallography, X-Ray
  • Male
  • Mice
  • Models, Molecular
  • Molecular Conformation
  • Pain / drug therapy
  • Pain Measurement / drug effects
  • Pyrrolidines / chemical synthesis*
  • Pyrrolidines / chemistry
  • Pyrrolidines / therapeutic use*

Substances

  • Analgesics
  • Pyrrolidines