1292943-25-9Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel dual FFA1 (GPR40)/PPARδ agonists as potential anti-diabetic agents
Li, Zheng,Hu, Lijun,Wang, Xuekun,Zhou, Zongtao,Deng, Liming,Xu, Yawen,Zhang, Luyong
, (2019/09/12)
The free fatty acid receptor 1 (FFA1) and peroxisome proliferator-activated receptor δ (PPARδ) were considered as potential anti-diabetic targets, and the dual FFA1/PPARδ agonists might provide synergistic effect in insulin secretion and sensibility. Herein, we further develop dual agonists by screening 7 series of heterocycles, resulting in the discovery of compound 19 with considerable oral pharmacokinetic profile. Compound 19 exhibited a balanced potency between FFA1 and PPARδ, and high selectivity over PPARα and PPARγ. Moreover, compound 19 exerted improved glucose-lowering effects and insulin sensitivity in a dose-dependent manner, which might be attributed to its dual effects to simultaneously regulate insulin secretion and resistance. Our results extended the existing chemical space, and provided a potent tool compound 19.
Steric and electronic factors influence regio-isomeric thiazole formations between substituted benzothioamides and ethyl bromopyruvate
Liang, Jun,Soucy, Valerie Dorman,Tusi, Vickie,Liu, Yanzhou,Zhang, Birong,Lai, Yingjie,Magnuson, Steve,Zhu, Bingyan,Wang, Fangdao,Gu, Jinghao,Zhang, Qingfen,Wu, Yuan,Deng, Wei,Yang, Wenqian
, p. 1137 - 1146 (2014/08/05)
We observed unexpected thiazole 1B formation when 2,6- dichlorobenzothioamide 1 and ethyl bromopyruvate were reacted under basic conditions at elevated temperatures in ethanol. Thiazole 1B, regio-isomeric to that expected under conventional Hantzsch condi
