Synthesis and structure-activity relationships of novel 2-amino alkyl chromones and related derivatives as a site-selective ligands

G Baziard-Mouysset, S Younes, Y Labssita…

Index: Baziard-Mouysset, Genevieve; Younes, Salouma; Labssita, Youssef; Payard, Marc; Caignard, Daniel-Henri; Rettori, Marie-Claire; Renard, Pierre; Pfeiffer, Bruno; Guardiola-Lemaitre, Beatrice European Journal of Medicinal Chemistry, 1998 , vol. 33, # 5 p. 339 - 347

Full Text: HTML

Citation Number: 17

Abstract

Starting from a random screening showing that 2-[(4-benzylpiperazinyl) methyl] chromone was a selective and potent sigma ligand, a series of analogues were synthesized. Introduction of a substituent on the chromone moiety, replacement of methy-lenes by carbonyl groups and benzyl by aryl groups decrease the affinity for sigma sites. The result obtained after introduction of various substituents on the aromatic part of the benzyl is ...