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Paper | Regular issue | Vol 85, No. 11, 2012, pp.2693-2712
Published online, 12th September, 2012
DOI: 10.3987/COM-12-12565
Design, Synthesis and Biological Activity Evaluation of 2,5-Diphenyl-1,3,4-oxadiazole Derivatives as Novel Inhibitors of Fructose-1,6-bisphosphatase

Hai-Bing He, Li-Xin Gao, Yue-Yang Zhou, Ting Liu, Jie Tang, Xue-Ping Gong, Wen-Wei Qiu, Jing-Ya Li,* Jia Li,* and Fan Yang*

*Shanghai Engineering Research Center of Molecular Theraputics and New Drug Development, East China Normal University, North Zhongshan Road, Shanghai 200062, China


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.