Benzyl prolinate derivatives as novel selective KCC2 blockers.

Benzyl prolinate derivatives as novel selective KCC2 blockers.

Bioorganic & medicinal chemistry letters (2010-03-20)

Cécile Pégurier, Nathalie Bosman, Philippe Collart, Marie-Laure Delporte, Karine Leclercq, Sébastien Lengelé, Ananda Kumar Kanduluru, Stéphane Meunier, Nathalie Pacico, Lakshmana Rao Vadali, Alain Wagner, Christian Wolff, Laurent Provins

PMID20299216

摘要

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.