| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375122 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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 R1 phenyl group improved the overall general profile of these prolinate derivatives.
Graphical abstractThe benzyl prolinate 13 has been identified as a potent KCC2 blocker with selectivity versus NKCC1 and favorable ADME properties. It was evaluated in an in vivo model of epilepsy, the audiogenic mouse seizure test.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,