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Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7. Epub 2006 Jan 24.

Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.

Author information

1
Pharma Division, Discovery Chemistry, F. Hoffman-La Roche Ltd, CH-4070 Basel, Switzerland.

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.

PMID:
16439120
DOI:
10.1016/j.bmcl.2005.12.088
[Indexed for MEDLINE]

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