Discovery of N

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• 作者：Zhijian Zhao ; William H. Leister ; Julie A. O’ ; Brien ; Wei Lemaire ; David L. Williams Jr. ; Marlene A. Jacobson ; Cyrille Sur ; Gene G. Kinney ; Doug J. Pettibone ; Philip R. Tiller ; Sheri Smith ; Georg
• 关键词：GlyT1 ; Schizophrenia ; NMDA receptor ; Inhibitor ; N-{ ; [1-(Propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 March 2009
• 年：2009
• 卷：19
• 期：5
• 页码：1488-1491
• 全文大小：2553 K

文摘

Employing an iterative analogue library approach, novel potent and selective glycine transporter 1 (GlyT1) inhibitors containing a 4-pyridin-2-ylpiperidine sulfonamide have been discovered. These inhibitors are devoid of time-dependent CYP inhibition activity and exhibit improved aqueous solubility versus the corresponding 4-phenylpiperidine analogues.