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7086770 
Journal Article 
DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2,5-DIPHENYL-1,3,4-OXADIAZOLE DERIVATIVES AS NOVEL INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE 
He, HaiB; Yang, Fan; Gao, LiXin; Zhou, YueY; Liu, T; Tang, Jie; Gong, XueP; Qiu, WenWei; Li, JYa; Li, Jia; , 
2012 
Yes 
Heterocycles
ISSN: 0385-5414 
PERGAMON-ELSEVIER SCIENCE LTD 
OXFORD 
2693-2712 
WOS:000311132900004 
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 mu M) 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.