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

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Abstract

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 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-HT(1A) sites with nanomolar affinity (IC50=1.5nM) and high selectivity over 5-HT(2A), 5-HT(2C), 5-HT3, D2, and D3 receptors. Copyright (C) 1999 Elsevier Science Ltd.

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Boyé, S., Pfeiffer, B., Renard, P., Rettori, M. C., Guillaumet, G., & Viaud, M. C. (1999). N,N-disubstituted aminomethyl benzofuran derivatives: Synthesis and preliminary binding evaluation. Bioorganic and Medicinal Chemistry, 7(2), 335–341. https://doi.org/10.1016/S0968-0896(98)00239-9

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