Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe

Further chemical optimization of the MLSCN/MLPCN probe ML077 (KCC2 IC(50) = 537 nM) proved to be challenging as the effort was characterized by steep SAR. However, a multidimensional iterative parallel synthesis approach proved productive. Herein we report the discovery and SAR of an improved novel...

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Main Authors: Delpire, Eric, Baranczak, Aleksandra, Waterson, Alex G., Kim, Kwangho, Kett, Nathan, Morrison, Ryan D., Daniels, J. Scott, Weaver, C. David, Lindsley, Craig W.
Format: Artigo
Sprog:Inglês
Udgivet: 2012
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC3389279/
https://ncbi.nlm.nih.gov/pubmed/22727639
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2012.05.126
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