N, N-Disubstituted Aminomethyl Benzofuran Derivatives: Synthesis and Preliminary Binding Evaluation

…, B Pfeiffer, P Renard, MC Rettori, G Guillaumet…

Index: Boye, Sophie; Pfeiffer, Bruno; Renard, Pierre; Rettori, Marie-Claire; Guillaumet, Gerald; Viaud, Marie-Claude Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 2 p. 335 - 341

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Citation Number: 9

Abstract

A series of new N-substituted 2, 3-dihydro-2-aminomethyl-2H-1-benzofuran derivatives was prepared and evaluated for affinity at 5-HT1A, 5-HT2A, 5-HT2C, 5-HT3, D2, and D3 receptors. 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-HT1A sites with nanomolar affinity (IC50= 1.5 nM) and high selectivity over 5-HT2A, 5-HT2C, 5-HT3, D2, ...