3,5-Diphenyl-1H-pyrazole derivatives. VIII. N-substituted 3-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)-propanamides, -propanamines and 2-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)ethanamines with platelet antiaggregating, hypotensive, antiarrhythmic and other activities

Farmaco. 1991 Mar;46(3):477-99.

Abstract

The synthesis of N,N-disubstituted 3-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)-propanamides and -propanamines, starting from 4-benzoyloxy-3,5-diphenyl-1H-pyrazole, and of N-substituted 2-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)ethanamines, starting from 4-acetoxy-1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole, is described. Some of the above compounds showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as moderate hypotensive, antiarrhythmic, local anesthetic, sedative and antiinflammatory activities in rats and mice.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anesthetics / chemical synthesis
  • Animals
  • Anti-Arrhythmia Agents / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Antihypertensive Agents / chemical synthesis*
  • Benzene Derivatives / chemical synthesis*
  • Benzene Derivatives / pharmacology
  • Humans
  • In Vitro Techniques
  • Mice
  • Motor Activity / drug effects
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology
  • Rats

Substances

  • Anesthetics
  • Anti-Arrhythmia Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antihypertensive Agents
  • Benzene Derivatives
  • Platelet Aggregation Inhibitors
  • Pyrazoles