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Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2009-01-09 , DOI: 10.1016/j.bmcl.2008.12.115 Zhijian Zhao , William H. Leister , Julie A. O’Brien , Wei Lemaire , David L. Williams , Marlene A. Jacobson , Cyrille Sur , Gene G. Kinney , Doug J. Pettibone , Philip R. Tiller , Sheri Smith , George D. Hartman , Craig W. Lindsley , Scott E. Wolkenberg
中文翻译：
的发现ñ - {[1-（丙基磺酰基）-4-吡啶-2-基哌啶-4-基]甲基}苯甲酰胺作为新的，选择性的和有效GlyT1抑制剂
更新日期：2009-01-09
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2009-01-09 , DOI: 10.1016/j.bmcl.2008.12.115 Zhijian Zhao , William H. Leister , Julie A. O’Brien , Wei Lemaire , David L. Williams , Marlene A. Jacobson , Cyrille Sur , Gene G. Kinney , Doug J. Pettibone , Philip R. Tiller , Sheri Smith , George D. Hartman , Craig W. Lindsley , Scott E. Wolkenberg
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.
中文翻译：
的发现ñ - {[1-（丙基磺酰基）-4-吡啶-2-基哌啶-4-基]甲基}苯甲酰胺作为新的，选择性的和有效GlyT1抑制剂
利用迭代类似物库方法，已发现了含有4-吡啶-2-基哌啶磺酰胺的新型有效且选择性的甘氨酸转运蛋白1（GlyT1）抑制剂。这些抑制剂没有时间依赖性的CYP抑制活性，并且与相应的4-苯基哌啶类似物相比表现出改善的水溶性。
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