1.
Bioorg Med Chem Lett
; 21(1): 497-501, 2011 Jan 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21075628
RESUMO
The discovery and structure-activity relationship of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 26i was found to be a high potency, selective cannabinoid CB(1) antagonist.
Assuntos
Amidas/química , Indóis/química , Receptor CB1 de Canabinoide/antagonistas & inibidores , Amidas/síntese química , Amidas/farmacocinética , Animais , Cães , Avaliação Pré-Clínica de Medicamentos , Indóis/síntese química , Indóis/farmacocinética , Masculino , Camundongos , Modelos Moleculares , Ratos , Ratos Wistar , Receptor CB1 de Canabinoide/metabolismo , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 21(10): 3163-7, 2011 May 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21458261
RESUMO
The discovery of a novel series of 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamide antagonists of the vasopressin V(1A) receptor is disclosed. Compounds 47 and 48 were found to be high affinity, selective vasopressin V(1A) antagonists.