Medicinal Chemistry Research

, Volume 14, Issue 2, pp 57–73

Benzimidazole, Benzoxazole and Benzothiazole Derivatives as 5HT2B Receptor Ligands. Synthesis and Preliminary Pharmacological Evaluation

  • G. Giorgioni
  • B. Accorroni
  • A. Di Stefano
  • G. Marucci
  • A. Siniscalchi
  • F. Claudi
Article

DOI: 10.1007/s00044-005-0125-z

Cite this article as:
Giorgioni, G., Accorroni, B., Di Stefano, A. et al. Med Chem Res (2005) 14: 57. doi:10.1007/s00044-005-0125-z

2-Phenethylbenzimidazole, 2-phenethylbenzoxazole and 2-phenethylbenzothiazole derivatives were synthesized to explore the structural features of the serotonin 5-HT2B receptor antagonists. Those molecules were designed to recognize the 5-HT2B receptor and to discriminate it from the 5-HT2A and 5-HT2C subtypes. All compounds were characterized by binding affinity determination for 5-HT2A and 5-HT2C subtypes and antagonistic activity for 5-HT2B receptor in rat stomach fundus. None of the new compounds showed affinity for 5-HT2A and 5-HT2C subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations.

Copyright information

© Birkhauser Boston 2005

Authors and Affiliations

  • G. Giorgioni
    • 1
  • B. Accorroni
    • 1
  • A. Di Stefano
    • 2
  • G. Marucci
    • 1
  • A. Siniscalchi
    • 3
  • F. Claudi
    • 1
  1. 1.Dipartimento di Scienze ChimicheUniversità di Camerino62032 Camerino (MC)Italy
  2. 2.Dipartimento di Scienze del FarmacoUniversità G. D'Annunzio66100 ChietiItaly
  3. 3.Dipartimento di Medicina Sperimentale e Clinica, Sezione di FarmacologiaUniversità di Ferrara44100 FerraraItaly

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