1.
Bioorg Med Chem Lett
; 12(20): 2957-61, 2002 Oct 21.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12270183
RESUMO
The synthesis and SAR of a series of human beta3 adrenoreceptor agonists based on a template derived from a common pharmacophore coupled with 4-aminomethylpiperidine is described. Potent and selective agents were identified such as 26 that was in vitro active in CHO cells expressing human beta3-AR (EC50=49 nM, IA=1.1), and in vivo active in a transgenic mouse model.
Assuntos
Agonistas de Receptores Adrenérgicos beta 3 , Agonistas Adrenérgicos beta/síntese química , Agonistas Adrenérgicos beta/farmacologia , Piperidinas/síntese química , Piperidinas/farmacologia , Animais , Células CHO , Cricetinae , Humanos , Indicadores e Reagentes , Camundongos , Camundongos Transgênicos , Receptores Adrenérgicos beta 3/genética , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 12(20): 2963-7, 2002 Oct 21.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12270184
RESUMO
The synthesis and SAR of a series of beta3 adrenoreceptor agonists based on a novel template derived from 4-aminomethylpiperidine coupled with a common pharmacophore, arylethylamine, is described. This combination led to the identification of human beta3 adrenoreceptor agonists with in vivo activity in a transgenic mouse model.