Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists

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.

Full text not available from this repository.

Official URL: http://edoc.unibas.ch/54628/

Downloads: Statistics Overview


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)
UniBasel Contributors:Huwyler, Jörg
Item Type:Article, refereed
Article Subtype:Research Article
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:27 Nov 2017 11:12
Deposited On:27 Nov 2017 11:12

Repository Staff Only: item control page