A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity

Bioorg Med Chem. 2013 Jul 1;21(13):3695-701. doi: 10.1016/j.bmc.2013.04.031. Epub 2013 Apr 26.

Abstract

We report the synthesis and bio-pharmacological evaluation of a class of pyrrole derivatives featuring a small appendage fragment (carbaldehyde, oxime, nitrile) on the central core. Compound 1c proved to be extremely effective in vivo, showing an interesting anti-nociceptic profile that is comparable to reference compounds already marketed, hence representing a great stimulus for a further improvement of this class of molecules.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / chemistry*
  • Analgesics / pharmacology
  • Analgesics / therapeutic use*
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use*
  • Cell Line
  • Cyclooxygenase 2 Inhibitors / chemistry
  • Cyclooxygenase 2 Inhibitors / pharmacology
  • Cyclooxygenase 2 Inhibitors / therapeutic use
  • Male
  • Mice
  • Pain / drug therapy
  • Pyrroles / chemistry*
  • Pyrroles / pharmacology
  • Pyrroles / therapeutic use*
  • Structure-Activity Relationship

Substances

  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase 2 Inhibitors
  • Pyrroles