新型、选择性且强效的甘氨酸转运体1（GlyT1）抑制剂N-{[1-(丙基磺酰基)-4-吡啶-2-基哌啶-4-基]甲基}苯甲酰胺的发现
Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.
作者信息
Zhao Zhijian, Leister William H, O'Brien Julie A, Lemaire Wei, Williams David L, Jacobson Marlene A, Sur Cyrille, Kinney Gene G, Pettibone Doug J, Tiller Philip R, Smith Sheri, Hartman George D, Lindsley Craig W, Wolkenberg Scott E
机构信息
Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., Inc., WP-14-1, PO Box 4 Sumneytown Pike, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1488-91. doi: 10.1016/j.bmcl.2008.12.115. Epub 2009 Jan 9.
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.
采用迭代模拟库方法，已发现含有4-吡啶-2-基哌啶磺酰胺的新型高效且选择性的甘氨酸转运体1（GlyT1）抑制剂。这些抑制剂没有时间依赖性的细胞色素P450抑制活性，并且与相应的4-苯基哌啶类似物相比，其水溶性有所提高。
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