1.
Bioorg Med Chem Lett
; 17(12): 3504-7, 2007 Jun 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17485206
RESUMO
A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT(6) receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT(6) receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hERG inhibition of this series of compounds is discussed.
Assuntos
Oxazinas/farmacologia , Receptores de Serotonina/efeitos dos fármacos , Antagonistas da Serotonina/farmacologia , Animais , Modelos Químicos , Oxazinas/síntese química , Ratos , Receptores de Serotonina/metabolismo , Antagonistas da Serotonina/síntese química , Relação Estrutura-Atividade
2.
