Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitro
- VernacularTitle:苯氧异丁酸类化合物的合成及其体外抗糖尿病活性
- Author:
Qingle ZENG
;
Heqing WANG
;
Huan LUO
;
Xiaoping GAO
;
Zhongrong LIU
;
Bogang LI
;
Fengpeng WANG
;
Yufen ZHAO
- Publication Type:Journal Article
- Keywords:
insulin sensitizers;
antidiabetic activity;
phenyloxyisobutyric acid derivatives;
3T3-L1adipocytes;
GOD-POD method
- From:
Acta Pharmaceutica Sinica
2006;41(2):108-114
- CountryChina
- Language:Chinese
-
Abstract:
Aim To design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds. Methods 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. Results In vitro insulin-sensitizing activity (3T3-L1adipocyte) demonstrated, that the cultured glucose concentration of up-clear solution detected with GODpioglitazone, compounds A and B were added to the insulin-resistant system. Conclusion 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.
