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

Authors
Boye, S Pfeiffer, B Renard, P Rettori, MC Guillaumet, G Viaud, MC
Citation
S. Boye et al., N,N-disubstituted aminomethyl benzofuran derivatives: Synthesis and preliminary binding evaluation, BIO MED CH, 7(2), 1999, pp. 335-341
Citations number
30
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
7
Issue
2
Year of publication
1999
Pages
335 - 341
Database
ISI
SICI code
0968-0896(199902)7:2<335:NABDSA>2.0.ZU;2-3
Abstract
A series of new N-substituted 2,3-dihydro-2-aminomethyl-2H-1-benzofuran der ivatives was prepared and evaluated for affinity at 5-HT1A, 5-HT2A, 5-HT2C, 5-H-3, D-2, and D-3 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 hi gh selectivity over 5-HT2A, 5-HT2C, 5-HT3, D-2, and D-3 receptors. (C) 1999 Elsevier Science Ltd. All rights reserved.