Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists

…, JU Peters, S Ceccarelli, S Kolczewski, E Vieira…

文献索引：Buettelmann, Bernd; Peters, Jens-Uwe; Ceccarelli, Simona; Kolczewski, Sabine; Vieira, Eric; Prinssen, Eric P.; Spooren, Will; Schuler, Franz; Huwyler, Joerg; Porter, Richard H. P.; Jaeschke, Georg Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 7 p. 1892 - 1897

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被引用次数: 10

摘要

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.