title: 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators.
abstract: A series of 6-aryl-3-pyrrolidinylpyridine analogs was explored as structurally novel negative allosteric modulators of the mGlu5 receptor lacking an alkyne or oxadiazole moiety. Compounds in this series were characterized by tractable SAR, good in vitro potencies and brain penetration in rodents.
authors.affiliation: Chemical & Pharmacokinetic Sciences, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA.
authors.forename: Jesse M
authors.initials: JM
authors.lastname: Weiss
authors.forename: Hermogenes N
authors.initials: HN
authors.lastname: Jimenez
authors.forename: Guiying
authors.initials: G
authors.lastname: Li
authors.forename: Myriam
authors.initials: M
authors.lastname: April
authors.forename: Michelle A
authors.initials: MA
authors.lastname: Uberti
authors.forename: Maria D
authors.initials: MD
authors.lastname: Bacolod
authors.forename: Robb M
authors.initials: RM
authors.lastname: Brodbeck
authors.forename: Darío
authors.initials: D
authors.lastname: Doller
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D057809:HEK293 Cells; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000097:blood; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D011725:Pyridines; D011759:Pyrrolidines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate