Issue 7, 2011

Discovery of novel selective Sigma-1 ligands as cognitive enhancers

Abstract

We disclose the identification and SAR of phenylcyclopropylcarboxamide compounds as novel, selective Sigma-1 ligands presenting excellent drug-like properties, high solubility and metabolic stability. A selected representative, compound 14, demonstrated in vivo very good brain exposure and antiamnesic effect in a mouse model of recognition memory.

Graphical abstract: Discovery of novel selective Sigma-1 ligands as cognitive enhancers

Article information

Article type
Concise Article
Submitted
14 Jan 2011
Accepted
10 May 2011
First published
10 Jun 2011

Med. Chem. Commun., 2011,2, 655-660

Discovery of novel selective Sigma-1 ligands as cognitive enhancers

A. Valade, S. B. Cross, C. Brown, E. Detrait, D. Ene, M. Gillard, M. Guyaux, Y. Lamberty, M. Maguire, N. Namdev, L. Provins, E. Schwartz and C. Vermeiren, Med. Chem. Commun., 2011, 2, 655 DOI: 10.1039/C1MD00010A

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