Büttelmann, Bernd and Peters, Jens-Uwe and Ceccarelli, Simona and Kolczewski, Sabine and Vieira, Eric and Prinssen, Eric P. and Spooren, Will and Schuler, Franz and Huwyler, Jörg and Porter, Richard H. P. and Jaeschke, Georg. (2006) Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 16 (7). pp. 1892-1897.
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Official URL: http://edoc.unibas.ch/54628/
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Abstract
Optimisation of affinity, chemical stability, metabolic stability and solubility led from a chemically labile HTS hit 1 to mGlu5 receptor antagonists (24-26) with high affinity for the allosteric MPEP binding site, improved microsomal metabolic stability and anxiolytic-like activity in vivo as assessed by the Vogel conflict drinking test.
| Faculties and Departments: | 05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmaceutical Technology (Huwyler) |
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| UniBasel Contributors: | Huwyler, Jörg |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | Elsevier |
| ISSN: | 0960-894X |
| e-ISSN: | 1464-3405 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Identification Number: |
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| Last Modified: | 27 Nov 2017 11:12 |
| Deposited On: | 27 Nov 2017 11:12 |
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