3,5-Diphenyl-1H-pyrazole derivatives. II--N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives with analgesic and other activities

Farmaco Sci. 1988 Dec;43(12):1019-34.

Abstract

The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / chemical synthesis*
  • Anesthetics, Local
  • Animals
  • Anti-Arrhythmia Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Blood Platelets / drug effects
  • Blood Platelets / metabolism
  • Blood Pressure / drug effects
  • Bromine / chemical synthesis
  • Bromine / pharmacology
  • Chemical Phenomena
  • Chemistry
  • Heart Rate / drug effects
  • Malondialdehyde / blood
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology
  • Rats

Substances

  • Analgesics
  • Anesthetics, Local
  • Anti-Arrhythmia Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Pyrazoles
  • Malondialdehyde
  • Bromine