New 1-arylindoles based serotonin 5-HT 7 antagonists. Synthesis and binding evaluation studies

C Sagnes, G Fournet, G Satala, AJ Bojarski…

Index: Sagnes, Charlene; Fournet, Guy; Satala, Grzegorz; Bojarski, Andrzej J.; Joseph, Benoit European Journal of Medicinal Chemistry, 2014 , vol. 75, p. 159 - 168

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Citation Number: 4

Abstract

Abstract Based on 5-HT 1A and 5-HT 7 ligand MR25003 scaffold, a new series of 1-aryl indole analogues were prepared and evaluated against 5-HT 7 receptors. Modulations of aryl moieties provided a large number of new indolic derivatives. Most of compounds tested have displayed 5-HT 7 affinity in the nanomolar range. Among them, 1-(naphthyl) indole derivative 3p (Ki (5-HT 7)= 4.5 nM) showed also a good selectivity over 5-HT 1A, 5-HT 2A ...