title: Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
abstract: We describe three novel regioisomeric series of aryl naphthyridine analogs, which are potent antagonists of the Class III GPCR mGlu5 receptor. The synthesis and in vitro and in vivo pharmacological activities of these analogs are discussed.
authors.affiliation: Department of Medicinal Chemistry, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
authors.forename: Paul
authors.initials: P
authors.lastname: Galatsis
authors.forename: Koji
authors.initials: K
authors.lastname: Yamagata
authors.forename: John A
authors.initials: JA
authors.lastname: Wendt
authors.forename: Cleo J
authors.initials: CJ
authors.lastname: Connolly
authors.forename: John W
authors.initials: JW
authors.lastname: Mickelson
authors.forename: Jared B J
authors.initials: JB
authors.lastname: Milbank
authors.forename: Susan E
authors.initials: SE
authors.lastname: Bove
authors.forename: Christopher S
authors.initials: CS
authors.lastname: Knauer
authors.forename: Rachel M
authors.initials: RM
authors.lastname: Brooker
authors.forename: Corinne E
authors.initials: CE
authors.lastname: Augelli-Szafran
authors.forename: Roy D
authors.initials: RD
authors.lastname: Schwarz
authors.forename: Jack J
authors.initials: JJ
authors.lastname: Kinsora
authors.forename: Kenneth S
authors.initials: KS
authors.lastname: Kilgore
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000502:physiology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D009287:Naphthyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate