Inhibitors of the glycine transporter type-2 (GlyT-2): synthesis and biological activity of benzoylpiperidine derivatives

RL Wolin, A Santillán, L Tang, C Huang, X Jiang…

文献索引：Wolin, Ronald L; Santillan Jr., Alejandro; Tang, Liu; Huang, Charles; Jiang, Xiaoxia; Lovenberg, Timothy W Bioorganic and medicinal chemistry, 2004 , vol. 12, # 16 p. 4511 - 4532

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被引用次数: 12

摘要

A series of benzoylpiperidine analogs related to 4a was prepared, and their ability to inhibit the uptake of [14C]-glycine in COS7 cells transfected with human glycine transporter type-2 (GlyT-2) was evaluated. Small structural changes to the benzoylpiperidine region of the molecule led to a significant decrease in GlyT-2 inhibitory activity. In contrast, the distal aryl ring was more tolerant to functional group modifications and could accommodate a variety ...