Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Synthesis and Biological Evaluation of Arylsulfonylpiperazine Derivatives as 5-HT6 Receptor Ligands

  • Jeon, Sun-Ah (Life Sciences Division, Korea Institute of Science and Technology) ;
  • Choo, Hyun-Ah (Life Sciences Division, Korea Institute of Science and Technology) ;
  • Park, Woo-Kyu (Pharmaceutical Screening Research Team, Korea Research Institute of Chemical Technology) ;
  • Rhim, Hye-Whon (Life Sciences Division, Korea Institute of Science and Technology) ;
  • Ko, Soo-Y. (Department of Chemistry, Ewha Womans University) ;
  • Cho, Yong-Seo (Life Sciences Division, Korea Institute of Science and Technology) ;
  • Koh, Hun-Yeong (Department of Chemistry, Inha University) ;
  • Pae, Ae-Nim (Life Sciences Division, Korea Institute of Science and Technology)
  • Published : 2007.02.20
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Abstract

The 5-HT6 antagonists are mainly related to the treatment of cognitive dysfunction or impairment associated with Alzheimer's disease and schizophrenia. There have been lots of efforts to develop 5-HT6 antagonists. As in our efforts, arylsulfonylpiperazine derivatives 1-3 were designed, synthesized and biologically evaluated against the human recombinant 5-HT6 serotonin receptor. Total 36 compounds were synthesized and the most active compound among the synthesized compounds is compound 2h with an IC50 value of 1.5 μM. The compound 2h is novel as 5-HT6 receptor ligand and could act as lead for the novel 5-HT6 receptor ligands.

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References

  1. Hoyer, D.; Clarke, D. E.; Fozard, J. R.; Hartig, P. R.; Martin, G. R.; Mylecharane, E. J.; Saxena, P. R.; Humphrey, P. P. Pharmacol. Rev. 1994, 46, 157
  2. Ruat, M.; Traiffort, E.; Arrang, J. M. Biochem. Biophys. Res. Commun. 1993, 193, 268 https://doi.org/10.1006/bbrc.1993.1619
  3. Meneses, A. Learn Memory 2003, 10, 363 https://doi.org/10.1101/lm.60503
  4. Meneses, A. Neurosci. Biobehav. Rev. 1999, 8, 1111
  5. Roth, B. L.; Hanizavareh, S. M.; Blum, A. E. Psychopharmacology 2004, 174, 17
  6. Vickers, S. P.; Dourish, C. T. Curr. Opin. Investig. Drugs 2004, 5, 377
  7. Holenz, J.; Pauwels, P. J.; Diaz, J. L.; Merce, R.; Codony, X.; Buschmann, H. Drug Discov. Today 2006, 11, 283 https://doi.org/10.1016/j.drudis.2006.02.004
  8. Drummond, A. H.; Bucher, F.; Levitan, I. B. Brain Research 1980, 184, 163 https://doi.org/10.1016/0006-8993(80)90595-8
  9. Drummond, A. H.; Bucher, F.; Levitan, I. B. J. Biol. Chem. 1980, 255, 6679

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