Synthesis, acute toxicity, analgesic activity and cytotoxicity of Some bisthiourea derivatives

Pak J Pharm Sci. 2017 Jul;30(4):1351-1356.

Abstract

Bisthiourea derivatives were synthesized by the reaction of benzoylisothiocyanate and diamines to give 1,2-Bis(N'-benzoylthioureidobenzene (1), 1,3-di(benzoylthioureido)benzene (2) and 1,4-di(benzoylthioureido)benzene (3) in acetone. Acute toxicity study revealed that LD50 of compound (1) and (3) is 120 mg/kg body weight. Visceral pain induced by injecting i.p acetic acid in mice were strongly inhibited by all the compounds. 94.65, 95.25 and 85.54% analgesic activity were observed in compounds (1), (2) and (3) at 15 mg/kg and (2) and (3) shows 97.63 and 96.42% at 30 mg/kg body weight respectively while (1) gives 100% analgesic activity. 100% cytotoxicity was observed in compounds (2) and (3) and 96% in compound (1) at 750 ppm. The results suggest that these compounds may have potential values for treatment of cancer and painful disorders.

MeSH terms

  • Acetic Acid
  • Analgesics / chemical synthesis*
  • Analgesics / pharmacology*
  • Animals
  • Artemia / drug effects
  • Dose-Response Relationship, Drug
  • Female
  • Lethal Dose 50
  • Male
  • Mice
  • Pain Measurement / drug effects*
  • Thiourea* / analogs & derivatives
  • Thiourea* / chemical synthesis
  • Thiourea* / pharmacology
  • Thiourea* / toxicity

Substances

  • Analgesics
  • Thiourea
  • Acetic Acid