Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

Céline Bonnefous; Jean-Michel Vernier; John H Hutchinson; Janice Chung; Grace Reyes-Manalo; Theodore Kamenecka

doi:10.1016/j.bmcl.2004.11.078

Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1197-200. doi: 10.1016/j.bmcl.2004.11.078.

Authors

Céline Bonnefous¹, Jean-Michel Vernier, John H Hutchinson, Janice Chung, Grace Reyes-Manalo, Theodore Kamenecka

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. [email protected]

PMID: 15686941
DOI: 10.1016/j.bmcl.2004.11.078

Abstract

The mGlu5 receptor has been implicated in a number of CNS disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amides as small molecules mGluR5 antagonists.

MeSH terms

Amides / chemical synthesis*
Amides / pharmacokinetics
Amides / pharmacology
Animals
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacokinetics
Enzyme Inhibitors / pharmacology
Humans
Hydrogen Bonding
Inhibitory Concentration 50
Pharmacokinetics
Pyridines / chemical synthesis
Pyridines / pharmacokinetics
Pyridines / pharmacology
Rats
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Amides
Enzyme Inhibitors
GRM5 protein, human
Grm5 protein, rat
Pyridines
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate