3,5-Diphenyl-1H-pyrazole derivatives. VII--Esters, 2-dialkylaminoethyl ethers and N-substituted carbamates of 1-(2-hydroxy-3-phenoxypropyl)-3,5-diphenyl-1H-pyrazole with depressant and platelet antiaggregating activities

Farmaco. 1990 May;45(5):527-43.

Abstract

The syntheses of 1-(2-hydroxy-3-phenoxypropyl)-3,5-diphenyl-1H-pyrazole 2 by reaction of 1-hydrazino-3-phenoxy-2-propranolol with dibenzoylmethane, of esters 3 and 2-dialkylaminoethyl ethers 4 starting from 2 as sodium salt and acyl chlorides or 2-chloroethyldialkylamines, respectively, as well as of N-aryl carbamates 5 by reaction of 2 with aryl isocyanates, are described. Some of the above compounds showed a considerable sedative effect in mice and a remarkable platelet antiaggregating activity in vitro, as well as moderate local anesthetic, analgesic and antiinflammatory activities in mice and rats.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anesthetics, Local / chemical synthesis
  • Animals
  • Anti-Arrhythmia Agents / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Antihypertensive Agents / chemical synthesis
  • Central Nervous System Depressants / chemical synthesis*
  • Chemical Phenomena
  • Chemistry
  • Humans
  • In Vitro Techniques
  • Mice
  • Motor Activity / drug effects
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology
  • Rats

Substances

  • Anesthetics, Local
  • Anti-Arrhythmia Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antihypertensive Agents
  • Central Nervous System Depressants
  • Platelet Aggregation Inhibitors
  • Pyrazoles