Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.

نویسندگان

  • Gianfabio Giorgioni
  • Dario Ambrosini
  • Cristian Vesprini
  • Alan Hudson
  • Cinzia Nasuti
  • Antonio Di Stefano
  • Piera Sozio
  • Osele Ciampi
  • Barbara Costa
  • Claudia Martini
  • Antonio Carrieri
  • Giuseppe Carbonara
  • Christoph Enzensperger
  • Maria Pigini
چکیده

Based on the well known biological versatility of the imidazoline nucleus, we prepared the novel derivatives 3a-k inspired by 2-BFI scaffold to assess imidazoline molecules as D(2)-like dopamine receptor ligands. Conservative chemical modifications of the lead structure, such as the introduction of an hydroxy group in the aromatic ring alone or associated with N-benzyl substitution, provided partial (3f) or nearly full (3e and 3h) agonists, all endowed with D(2)-like potency comparable to that of dopamine.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry

دوره 18 19  شماره 

صفحات  -

تاریخ انتشار 2010