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Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel,selective and potent GlyT1 inhibitors |
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| Authors: | 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 |
| Institution: | 1. Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., Inc., WP-14-1, PO Box 4 Sumneytown Pike, West Point, PA 19486, USA;2. Department of Neuroscience, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA;3. Department of Drug Metabolism, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA |
| Abstract: | 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. |
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