95016-23-2Relevant 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.
Synthesis and biological activity of 2-(bis((1,3,4-oxadiazolyl/1,3,4- thiadiazolyl)methylthio)methylene)malononitriles
Padmavathi,Dinneswara Reddy,Nagi Reddy,Mahesh
experimental part, p. 1367 - 1373 (2011/04/24)
The reactivity of ketene dithiolates in the presence of different equivalents of sodium ethoxide was studied. 2-(Bis((5-aryl-1,3,4-oxadiazol-2-yl) methylthio)methylene)malononitriles 5 and 2-(bis((5-aryl-1,3,4-thiadiazol-2-yl) methylthio)methylene)malononitriles 6 were prepared by the reaction of malononitrile with carbon disulfide and 5-aryl-2-(chloromethyl)-1,3,4- oxadiazoles 3/5-aryl-2-(chloromethyl)-1,3,4-thiadiazoles 4. The preliminary antimicrobial and antioxidant activities of the lead compounds were assayed.
One-pot synthesis of 5-{[Bis(azolylmethylthio)]methylene}pyrimidine-2,4,6- (1H,3H,5H)-triones
Padmavathi, Venkatapuram,Reddy, Guda Dinneswara,Venkatesh, Bhumireddy Chinnachennaiahgari,Padmaja, Adivireddy
body text, p. 165 - 169 (2011/10/05)
A new class of hitherto unknown trisheterocycles, bisoxadiazolyl/ bisthiadiazolyl pyrimidinetriones/thioxopyrimidinediones was prepared in a one-pot reaction and their antimicrobial activity was studied.
