Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitro / 药学学报

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>