
pmid: 20299216
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.
Structure-Activity Relationship, Proline, Symporters, K Cl- Cotransporters, Animals, Stereoisomerism, Rats
Structure-Activity Relationship, Proline, Symporters, K Cl- Cotransporters, Animals, Stereoisomerism, Rats
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