Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitro / 药学学报
Acta Pharmaceutica Sinica
; (12): 108-114, 2006.
Article
em Zh
| WPRIM
| ID: wpr-253490
Biblioteca responsável:
WPRO
ABSTRACT
<p><b>AIM</b>To design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds.</p><p><b>METHODS</b>Eight new target compounds were synthesized by combination of lipophilic moieties and acidic moiety with nucleophilic replacement or Mitsunobu condensation. The eight compounds were confirmed by 1H NMR, 13C NMR, IR and MS.</p><p><b>RESULTS</b>In vitro insulin-sensitizing activity (3T3-L1 adipocyte) demonstrated, that the cultured glucose concentration of up-clear solution detected with GOD-POD assay were 5.942, 6.339, 6.226 and 6.512 mmol x L(-1), respectively, when rosiglitazone, pioglitazone, compounds A and B were added to the insulin-resistant system.</p><p><b>CONCLUSION</b>In vitro insulin-sensitizing activity of target compound A is in between that of rosiglitazone and pioglitazone, and activity of target compound B is slightly less than that of pioglitazone.</p>
Texto completo:
1
Índice:
WPRIM
Assunto principal:
Farmacologia
/
Butiratos
/
Estrutura Molecular
/
Química
/
Adipócitos
/
Células 3T3-L1
/
PPAR gama
/
Hipoglicemiantes
/
Insulina
Limite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2006
Tipo de documento:
Article