发现N-（2-芳基环己基）取代的螺哌啶类化合物作为一类新型甘氨酸转运体1（GlyT1）抑制剂。
Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.
作者信息
Pinard Emmanuel, Ceccarelli Simona M, Stalder Henri, Alberati Daniela
机构信息
F. Hoffmann-La Roche Ltd, Pharmaceutical Research Basel, Discovery Chemistry, CH-4070 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2006 Jan 15;16(2):349-53. doi: 10.1016/j.bmcl.2005.09.075. Epub 2005 Oct 21.
PMID:16246557
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.
摘要
对罗氏化合物库进行筛选后，确定顺式-N-(2-苯基-环己基)-螺哌啶1为结构新颖的甘氨酸转运体1（GlyT1）抑制剂。在该系列中开展的构效关系研究，促成了对甘氨酸转运体2（GlyT2）亚型具有优异选择性的高效化合物的发现。
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