Design, synthesis, and in-vivo pharmacological screening of N,3-(substituted diphenyl)-5-phenyl-1H-pyrazoline-1-carbothioamide derivatives

Arch Pharm (Weinheim). 2009 Mar;342(3):173-81. doi: 10.1002/ardp.200800130.

Abstract

Various 3,5-(substituted diphenyl)-4,5-dihydro-pyrazole-1-carbothioic acid phenylamides were synthesized starting from substituted acetophenones. Structures of the compounds were confirmed on the basis of spectral data. The compounds were evaluated for their anticonvulsant and antidepressant activity. Interestingly, out of 26 compounds, four (3f, 3g, 3t, and 3u) were found to protect 100% of the animals in the MES screen at a dose of 25 mg/kg. They were also found to have appreciable anticonvulsant activity in scPTZ screen. Two compounds, 3j and 3o, significantly reduced the duration of the immobility time at 25 mg/kg dose, when compared to control.

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology
  • Antidepressive Agents / chemical synthesis*
  • Antidepressive Agents / pharmacology
  • Drug Evaluation, Preclinical
  • Mice
  • Molecular Structure
  • Neurotoxicity Syndromes
  • Pyrazoles
  • Thioamides / administration & dosage
  • Thioamides / adverse effects
  • Thioamides / chemical synthesis*

Substances

  • Anticonvulsants
  • Antidepressive Agents
  • Pyrazoles
  • Thioamides