Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives

Authors

  • Farhad Gharebaghi Department of Medicinal Chemistry, School of Pharmacy, Zanjan University of Medical Sciences. Zanjan, Iran
  • Farzad Kobarfard Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  • Marjan Esfahani Zadeh Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  • Maryam Hashemi Department of Medicinal Chemistry, School of Pharmacy, Zanjan University of Medical Sciences. Zanjan, Iran
  • Shohreh Mohebbi Department of medicinal chemistry, school of pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
  • Vida Mashayekhi Department of Pharmaceutical Biotechnology, School of Pharmacy, Zanjan University of Medical Sciences. Zanjan, Iran
Abstract:

A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet aggregation. Based on the results, substituted phenylhydrazones showed promising activity. Among them, compound 1i was the most potent derivative with an IC50 comparable to that of indomethacin as a standard drug. The hydrazone derivatives were also tested for their cytotoxicity using on platelet concentrates and fibroblast L929 cells. The majority of the derivatives showed an acceptable selectivity towards antiplatelet aggregation activity. Based on the activity data, phenylhydrazone derivatives (1a-i) exhibited considerable antiplatelet activity and minimal toxic effect on platelet cells. The results of the present study could provide a better understanding of the structure activity relationship of antiplatelet indolehydrazones.

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Journal title

volume 14  issue 4

pages  1077- 1086

publication date 2015-10-01

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