Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.
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.
Wendt
John A
JA
Department of Medicinal Chemistry, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
Deeter
Susan D
SD
Bove
Susan E
SE
Knauer
Christopher S
CS
Brooker
Rachel M
RM
Augelli-Szafran
Corinne E
CE
Schwarz
Roy D
RD
Kinsora
Jack J
JJ
Kilgore
Kenneth S
KS
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
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