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Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists
Journal
Bioorganic and Medicinal Chemistry Letters
Volume
16
Number
7
Pages / Article-Number
1892-7
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.
