title: Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.
abstract: A novel series of potent 2-aryl pyrido[2,3-d]pyrimidine mGlu5 receptor antagonists are described. The synthesis and 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: John A
authors.initials: JA
authors.lastname: Wendt
authors.forename: Susan D
authors.initials: SD
authors.lastname: Deeter
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; D002118:Calcium / Q000378:metabolism; D006224:Cricetinae; D003412:Cricetulus; D052246:Cyclooxygenase 2 Inhibitors / Q000627:therapeutic use; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007596:Joints / Q000473:pathology; D007783:Lactones / Q000627:therapeutic use; D010003:Osteoarthritis / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000627:therapeutic use
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D018691:Excitatory Amino Acid Antagonists; D007202:Indicators and Reagents; D007783:Lactones; D011725:Pyridines; D011743:Pyrimidines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate; D013450:Sulfones; C116926:rofecoxib; C121465:6-methyl-2-(phenylethynyl)pyridine; D002118:Calcium