Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzami des as novel, selective and potent GlyT1 inhibitors
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...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2009-03, Vol.19 (5), p.1488-1491 |
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| container_end_page | 1491 |
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| container_issue | 5 |
| container_start_page | 1488 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 19 |
| creator | 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 |
| description | 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. |
| doi_str_mv | 10.1016/j.bmcl.2008.12.115 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (5), p.1488-1491 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_20472852 |
| source | Elsevier ScienceDirect Journals |
| title | Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzami des as novel, selective and potent GlyT1 inhibitors |
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