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Aim:To synthesize and study the anti-diabetic activity of (RS)-2-ethoxy-3-{4-[2-(4-trifluoromethanesulfonyloxy-phenyl)-ethoxy]-phenyl}-propionic acid(compound Ⅰ).Methods:Compound Ⅰ was prepared in 6 steps,using 4-(2-hy-droxy-ethyl)-phenol as the starting material.The in vitro selectivity and potencyof target compound Ⅰ,rosiglitazone and WY-14643 on human PPARα and PPARγwere determined in reporter gene assays.In vivo,rosiglitazone and compound Ⅰwere administered orally to KK~(Ay) mice for 14d.Insulin tolerance tests and oralglucose tolerance tests were performed on the 10th and 14th day of treatment,respectively.At the end of the treatment,sera were collected for biochemicalanalysis.Results:In vitro,compound Ⅰ significantly activated both PPARα andPPARγ.In vivo,compound Ⅰ corrected the impaired insulin and glucose toleranceof KK~(Ay) mice,and produced a significant reduction in plasma triglyceride levelsafter 14d of treatment.The effect produced was significant compared with thecontrol group.Conclusion:Both in vitro and in vivo anti-diabetic activity studiesfor compound Ⅰ were conducted and the data suggest that this compound is apotentially effective anti-diabetic agent.
Aim: To synthesize and study the anti-diabetic activity of (RS) -2-ethoxy-3- [4- (2- trifluoromethanesulfonyloxy-phenyl) -ethoxy] -phenyl} -propionic acid (compound I) : Compound I was prepared in 6 steps, using 4- (2-hy-droxy-ethyl) -phenol as the starting material. The in vitro selectivity and potency of target compound I, rosiglitazone and WY- 14643 on human PPARα and PPARγ content determined in reporter gene assays. In vivo, rosiglitazone and compound I were administered orally to KK ~ (Ay) mice for 14d. Insulin tolerance tests and oral glucose tolerance tests were performed on the 10th and 14th day of treatment, respectively. At the end of the treatment, sera were collected for biochemicalanalysis. Results: In vitro, compound Ⅰ significantly activated both PPARα and PPARγ.In vivo, compound Ⅰ corrected the impaired insulin and glucose tolerance of KK ~ (Ay) mice, and produced a significant reduction in plasma triglyceride levels after 14d of treatment The effect produced was significant compared with thecontrol group. Conflusion: Both in vitro and in vivo anti-diabetic activity studies for compound I were conducted and the data suggest that this compound is apotentially effective anti-diabetic agent.