Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
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.
Galatsis
Paul
P
Department of Medicinal Chemistry, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
Yamagata
Koji
K
Wendt
John A
JA
Connolly
Cleo J
CJ
Mickelson
John W
JW
Milbank
Jared B J
JB
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; 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
D009287:Naphthyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate