Benzyl prolinate derivatives as novel selective KCC2 blockers.
Fiche publication
Date publication
avril 2010
Auteurs
Membres identifiés du Cancéropôle Est :
Dr WAGNER Alain
Tous les auteurs :
Pegurier C, Bosman N, Collart P, Delporte ML, Leclercq K, Lengele S, Kanduluru AK, Meunier S, Pacico N, Vadali LR, Wagner A, Wolff C, Provins L
Lien Pubmed
Résumé
The discovery and optimization of a novel class of selective submicromolar KCC2 blockers is described. Details of synthesis and SAR are given together with ADME properties of selected compounds. A methylsulfone residue on the R(1) phenyl group improved the overall general profile of these prolinate derivatives.
Référence
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2542-5