N,N-disubstituted aminomethyl benzofuran derivatives: Synthesis and preliminary binding evaluation

  • Boyé S
  • Pfeiffer B
  • Renard P
 et al. 
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A series of new N-substituted 2,3-dihydro-2-aminomethyl-2H-1-benzofuran derivatives was prepared and evaluated for affinity at 5-HT(1A), 5-HT(2A), 5-HT(2C), 5-HT3, D2, and D3receptors. Compound 9, 8-[4-[N-propyl-N-(7-hydroxy-2,3-dihydro-2H-1-benzofuran-2-yl)methyl]aminobutyl]-8-azaspiro[4,5]decane-7,9-dione, bound at 5-HT(1A) sites with nanomolar affinity (IC50=1.5nM) and high selectivity over 5-HT(2A), 5-HT(2C), 5-HT3, D2, and D3receptors. Copyright (C) 1999 Elsevier Science Ltd.

Author-supplied keywords

  • 2,3-Dihydro-2-aminomethyl-2H-1-benzofurans
  • Ring contraction
  • Serotoninergic and dopaminergic receptor binding

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  • Sophie Boyé

  • Bruno Pfeiffer

  • Pierre Renard

  • Marie Claire Rettori

  • Gérald Guillaumet

  • Marie Claude Viaud

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