[Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitro].
OBJECTIVE
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-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.


CONCLUSIONS
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.
Zeng
Qing-le
QL
Department of Chemistry and Key Laboratory for Chemical Biology of Fujian Province, Xiamen University, Xiamen 361005, China. qlzeng@xmu.edu.cn
Wang
He-qing
HQ
Luo
Huan
H
Gao
Xiao-ping
XP
Liu
Zhong-rong
ZR
Li
Bo-gang
BG
Wang
Feng-peng
FP
Zhao
Yu-fen
YF