Thiosemicarbazone and thiazolylhydrazones of 1-indanone: As a new class of nonacidic anti-inflammatory and antiplatelet aggregation agents

Pak J Pharm Sci. 2019 Jan;32(1):15-19.

Abstract

This research based on the anti-inflammatory and antiplatelet aggregation properties of some new thiazolyl hydrazone derivatives of 1-indanone. In this regard a thiosemicabazone and twelve thiazolyl derivatives of 1-indanone have been synthesized. Out of these synthetic compounds seven derivatives 1-3, 6, 11-13 exhibited varying degree of anti-inflammatory action with IC50 esteems going from 5.1±1.3 - 78.8±4.6μM/mL. Compound 1 (IC50 =5.1±1.9μM) displayed potent result than standard ibuprofen (IC50 = 11.2±1.9 μM). In antiplatelet aggregation assay, five compounds 1, 5, 6, 8 and 11 were observed to be dynamic with IC50 esteems observed in the range of 38.34-255.7±4.1μM, wher eas, aspirin (IC50 = 30.3±2.6 μM) was used as standard. However, compound 11 was found to be good active for both anti-inflammatory and antiplatelet aggregation activities (IC50 = 13.9±4.9μg/mL) (IC50 = 38.60±3.1μM), respectively.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Inflammatory Agents / chemical synthesis
  • Anti-Inflammatory Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Humans
  • Hydrazones / chemical synthesis
  • Hydrazones / pharmacology*
  • Ibuprofen / pharmacology
  • Indans / chemical synthesis
  • Indans / pharmacology*
  • Molecular Structure
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / chemical synthesis
  • Platelet Aggregation Inhibitors / pharmacology*
  • Respiratory Burst / drug effects*
  • Structure-Activity Relationship
  • Thiosemicarbazones / chemical synthesis

Substances

  • Anti-Inflammatory Agents
  • Hydrazones
  • Indans
  • Platelet Aggregation Inhibitors
  • Thiosemicarbazones
  • Ibuprofen