Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors

E Pinard, SM Ceccarelli, H Stalder, D Alberati

Index: Pinard, Emmanuel; Ceccarelli, Simona M.; Stalder, Henri; Alberati, Daniela Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 2 p. 349 - 353

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Citation Number: 25

Abstract

Screening of the Roche compound library led to the identification of cis-N-(2-phenyl- cyclohexyl)-spiropiperidine 1 as structurally novel GlyT1 inhibitor. The SAR, which was developed in this series, resulted in the discovery of highly potent compounds displaying excellent selectivity against the GlyT2 isoform.

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