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Bioorg Med Chem Lett. 2010 Jan 1;20(1):184-8. doi: 10.1016/j.bmcl.2009.11.001. Epub 2009 Nov 5.

Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.

Author information

1
Novartis Institutes for Biomedical Research, Global Discovery Chemistry, Basel CH-4002, Switzerland.

Abstract

High throughput screening led to the identification of nicotinamide derivative 2 as a structurally novel mGluR5 antagonist. Optimization of the modular scaffold led to the discovery of 16m, a compound with high affinity for mGluR5 and excellent selectivity over other glutamate receptors. Compound 16m exhibits a favorable PK profile in rats, robust anxiolytic-like effects in three different animal models of fear and anxiety, as well as a good PK/PD correlation.

PMID:
19931453
DOI:
10.1016/j.bmcl.2009.11.001
[Indexed for MEDLINE]

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