Literature DB >> 20299216

Benzyl prolinate derivatives as novel selective KCC2 blockers.

Cécile Pégurier1, 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.   

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. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20299216     DOI: 10.1016/j.bmcl.2010.02.092

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Challenges of Finding Novel Drugs Targeting the K-Cl Cotransporter.

Authors:  Eric Delpire; C David Weaver
Journal:  ACS Chem Neurosci       Date:  2016-11-08       Impact factor: 4.418

Review 2.  Advances in the development of novel compounds targeting cation-chloride cotransporter physiology.

Authors:  Eric Delpire
Journal:  Am J Physiol Cell Physiol       Date:  2020-12-23       Impact factor: 5.282

  2 in total

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