title: Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. celine_bonnefous@merck.com
authors.forename: Céline
authors.initials: C
authors.lastname: Bonnefous
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Vernier
authors.forename: John H
authors.initials: JH
authors.lastname: Hutchinson
authors.forename: Janice
authors.initials: J
authors.lastname: Chung
authors.forename: Grace
authors.initials: G
authors.lastname: Reyes-Manalo
authors.forename: Theodore
authors.initials: T
authors.lastname: Kamenecka
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D006860:Hydrogen Bonding; D020128:Inhibitory Concentration 50; D010599:Pharmacokinetics; D011725:Pyridines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D004791:Enzyme Inhibitors; C578935:GRM5 protein, human; C578937:Grm5 protein, rat; D011725:Pyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate