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Benzyl prolinate derivatives as novel selective KCC2 blockers |
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| 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 |
| Affiliation: | 1. UCB Pharma SA, UCB NewMedicines, Chemin du Foriest, B-1420 Braine-L’Alleud, Belgium;2. Laboratoire des systèmes chimiques fonctionnels, UMR 7199 associé au CNRS, Faculté de Pharmacie, Université de Strasbourg, 74 route du Rhin, BP 24, F-67401 Illkirch, France |
| 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. |
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