Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ 1 ligands. Part 2

…, P Gilleron, MA Debreu-Fontaine, C Sergheraert…

Index: Gassiot, Amaury Cazenave; Charton, Julie; Girault-Mizzi, Sophie; Gilleron, Pauline; Debreu-Fontaine, Marie-Ange; Sergheraert, Christian; Melnyk, Patricia Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 21 p. 4828 - 4832

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Citation Number: 11

Abstract

Herein is described a new class of selective σ1 ligands consisting of tetrahydroisoquinoline- hydantoin (Tic-hydantoin) derivatives. Compound 1a has high affinity (IC50= 16nM) for σ1 receptor and is selective in a large panel of therapeutic targets. This study presents structural changes on the side chain of the Tic-hydantoin core. Analogs of higher affinity could be identified (IC50≈ 2–3nM).

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