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Bioorganic & medicinal chemistry letters

Benzyl prolinate derivatives as novel selective KCC2 blockers.


PMID 20299216

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.