1.
Bioorg Med Chem Lett
; 17(23): 6525-8, 2007 Dec 01.
Article
in English
| MEDLINE
| ID: mdl-17936624
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.
Subject(s)
Naphthyridines/chemical synthesis , Naphthyridines/pharmacology , Receptors, Metabotropic Glutamate/antagonists & inhibitors , Animals , CHO Cells , Cricetinae , Cricetulus , Rats , Receptor, Metabotropic Glutamate 5 , Receptors, Metabotropic Glutamate/physiology , Stereoisomerism , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 17(19): 5396-9, 2007 Oct 01.
Article
in English
| MEDLINE
| ID: mdl-17723296
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.