Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 1
Bioorganic & Medicinal Chemistry Letters(2005)
摘要
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).
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关键词
Hydantoin,Tic,σ receptors,Selectivity
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