Benzyl prolinate derivatives as novel selective KCC2 blockers

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2542-5. doi: 10.1016/j.bmcl.2010.02.092.
Cécile Pégurier  1 ,  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
Affiliations
  • 1. UCB Pharma SA, UCB NewMedicines, Chemin du Foriest, B-1420 Braine-L'Alleud, Belgium.
PMID: 20299216 DOI: 10.1016/j.bmcl.2010.02.092
Abstract

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.

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