Synthesis of novel beta-aminoalcohols containing nabumetone moiety with potential antidiabetic activity / 药学学报
Acta Pharmaceutica Sinica
;
(12): 412-421, 2011.
Artigo
em Chinês
| WPRIM
| ID: wpr-348939
ABSTRACT
Twenty five new beta-aminoalcohols containing nabumetone moiety were prepared via the reduction of potassium borohydride with a convenient and efficient procedure, starting from beta-aminoketones that have been synthesized by our group. Their chemical structures were determined by IR, MS, 1H NMR, 13C NMR, HR-MS and antidiabetic activities were screened in vitro. Preliminary results revealed that the antidiabetic activity of most beta-aminoalcohols were better than that of the corresponding beta-aminoketones. Although most compounds showed weak antidiabetic activity, the alpha-glucosidase inhibitory activity of compounds 5hd(1) and 5id(2) reached 74.37% and 90.15%, respectively, which were superior to the positive control. The relative peroxisome proliferator-activated receptor response element (PPRE) activity of five compounds were more than 60%, among them compound 5ca possessed the highest activity (112.59%). As lead molecules of antidiabetic agents, compounds 5hd(1), 5id(2) and 5ca deserve further study.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Butanonas
/
Química
/
Elementos de Resposta
/
Receptores Ativados por Proliferador de Peroxissomo
/
Inibidores de Ciclo-Oxigenase 2
/
Alfa-Glucosidases
/
Inibidores de Glicosídeo Hidrolases
/
Amino Álcoois
/
Hipoglicemiantes
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2011
Tipo de documento:
Artigo
Similares
MEDLINE
...
LILACS
LIS