Referenced in: none

Automatically associated channels: Kv11.1

Title: Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors.

Authors: Emmanuel Pinard, Daniela Alberati, Markus Bender, Edilio Borroni, Virginie Brom, Serge Burner, Holger Fischer, Dominik Hainzl, Remy Halm, Nicole Hauser, Synèse Jolidon, Judith Lengyel, Hans-Peter Marty, Thierry Meyer, Jean-Luc Moreau, Roland Mory, Robert Narquizian, Roger D Norcross, Philipp Schmid, Roger Wermuth, Daniel Zimmerli

Journal, date & volume: Bioorg. Med. Chem. Lett., 2010 Dec 1 , 20, 6960-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20974532

Abstract
Benzoylisoindolines were discovered as a novel structural class of GlyT1 inhibitors. SAR studies and subsequent lead optimization efforts focused primarily on addressing hERG liability and on improving in vivo efficacy resulted in the identification of potent GlyT1 inhibitors displaying excellent selectivity and in vivo PD and PK profiles.