Opening book details…
Can I read Sigma-1 ligands: Tic-hydantoin as a key pharmacophore on EtoBox?
Sigma-1 ligands: Tic-hydantoin as a key pharmacophore by Marion Toussaint; Deborah Mousset; Catherine Foulon; Ulrich Jacquemard; Claude Vaccher; Patricia Melnyk is a Chemistry article available to read on EtoBox.
What is Sigma-1 ligands: Tic-hydantoin as a key pharmacophore about?
## a b s t r a c t 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 Tichydantoin 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.
Who reads Sigma-1 ligands: Tic-hydantoin as a key pharmacophore?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Marion Toussaint; Deborah Mousset; Catherine Foulon; Ulrich Jacquemard; Claude Vaccher; Patricia Melnyk
- Publisher
- Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)
- Published
- 2010
- Language
- EN
- Field
- Chemistry (Physical Sciences)