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- W2000598080 abstract "Sigma-1 receptors are involved in numerous pathological dysfunctions and the synthesis of selective ligands is of interest. We identified a fused tetrahydroisoquinoline-hydantoin (Tic-hydantoin) structure with high affinity and selectivity for these receptors. We report here our efforts towards the pharmacomodulation of this substructure, the synthesis of 9 analogs with stereochemistry inversion, opening of isoquinoline ring, removal of isoquinoline nitrogen, replacement of isoquinoline by pyridine, of Tic-hydantoin moiety by quinazolinedione heterocycle. All these analogs provided a loss in the affinity for the sigma-1 receptor. The present work underlines the real importance of the Tic-hydantoin moiety for the obtainment of high affinity ligands." @default.
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- W2000598080 date "2010-01-01" @default.
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- W2000598080 title "Sigma-1 ligands: Tic-hydantoin as a key pharmacophore" @default.
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- W2000598080 doi "https://doi.org/10.1016/j.ejmech.2009.10.004" @default.
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