Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ 1 ligands. Part 1

…, S Girault-Mizzi, MA Debreu-Fontaine, P Melnyk…

Index: Charton, Julie; Gassiot, Amaury Cazenave; Girault-Mizzi, Sophie; Debreu-Fontaine, Marie-Ange; Melnyk, Patricia; Sergheraert, Christian Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 21 p. 4833 - 4837

Full Text: HTML

Citation Number: 16

Abstract

Herein is described a new class of selective σ1 ligands consisting of tetrahydroisoquinoline- hydantoin (Tic-hydantoin) derivatives. Compound 3a has high affinity (IC50= 16nM) for the σ1 receptor and is selective in a large panel of therapeutic targets. This first study presents structural changes around the Tic-hydantoin core, leading to a Tic-hydantoin analogue with a higher σ1 affinity (IC50≈ 1nM).