1.
Bioorg Med Chem Lett
; 17(23): 6525-8, 2007 Dec 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17936624
RESUMO
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.
Assuntos
Naftiridinas/síntese química , Naftiridinas/farmacologia , Receptores de Glutamato Metabotrópico/antagonistas & inibidores , Animais , Células CHO , Cricetinae , Cricetulus , Ratos , Receptor de Glutamato Metabotrópico 5 , Receptores de Glutamato Metabotrópico/fisiologia , Estereoisomerismo , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 17(16): 4599-603, 2007 Aug 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17562362
RESUMO
It has been hypothesized that peripherally restricted NMDA receptor antagonists may be effective analgesics for osteoarthritis pain. A class of novel quinoxalinedione atropisomers, first discovered for an NMDA receptor antagonist program for the treatment of stroke, was evaluated and further optimized with the goal of finding peripherally restricted NMDA receptor antagonists.