831215-29-3Relevant academic research and scientific papers
Design, synthesis and biological activity evaluation of 2,5-diphenyl-1,3,4-oxadiazole derivatives as novel inhibitors of fructose-1,6-bisphosphatase
He, Hai-Bing,Gao, Li-Xin,Zhou, Yue-Yang,Liu, Ting,Tang, Jie,Gong, Xue-Ping,Qiu, Wen-Wei,Li, Jing-Ya,Li, Jia,Yang, Fan
, p. 2693 - 2712 (2013/01/15)
Fructose-1,6-bisphosphatase (FBPase), an important gluconeogenic enzyme, catalyzes the hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate. The effort to discover new FBPase inhibitors was carried out by high-throughput screening (HTS) of a library of 56,000 lead-like compounds, and a 2,5-diphenyl-1,3,4-oxadiazole (3a, IC50 = 15.45 μM) which bearing no phosphate group was identified as a potential FBPase inhibitor for the first time. Structure-activity-relationship (SAR) research of a series of analogues obtained by modifying the substituent groups and replacing the 1,3,4-oxadiazole with several other heterocycles disclosed the key structure and substituent groups related to the binding with FBPase.
