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DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2,5-DIPHENYL-1,3,4-OXADIAZOLE DERIVATIVES AS NOVEL INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE

文献类型：期刊论文

作者He, Hai-Bing3; Gao, Li-Xin2; Zhou, Yue-Yang2; Liu, Ting1,4; Tang, Jie3; Gong, Xue-Ping1,4; Qiu, Wen-Wei1,4; Li, Jing-Ya2; Li, Jia2; Yang, Fan1,3,4
刊名HETEROCYCLES
出版日期2012-11-01
卷号85期号:11页码:2693-2712
关键词Fructose-1,6-bisphosphatase 2,5-Phenyl-1,3,4-oxadiazole Type-2 Diabetes Enzyme Inhibition
ISSN号0385-5414
DOI10.3987/COM-12-12565
文献子类Article
英文摘要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.
WOS关键词FRUCTOSE 1,6-BISPHOSPHATASE ; FBPASE INHIBITORS ; DISCOVERY ; POTENT ; ANALOGS ; GLUCONEOGENESIS ; EXPRESSION ; PRODRUGS ; SERIES ; LIVER
资助项目National Nature Science Foundation of China[81125023] ; Shanghai Science and Technology council[11DZ2292200] ; Shanghai Science and Technology Council[10142200800] ; National Science and Technology Major Projects for Major New Drugs Innovation and Development[2012ZX09304011] ; National Science and Technology Major Projects for Major New Drugs Innovation and Development[2012ZX09301-001-004] ; Chinese Academy of Sciences[KSCS2-EW-R-15] ; Laboratory of Organic Functional Molecules, Sino-French Institute of ECNU[00000000]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000311132900004
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/277891]  
专题国家新药筛选中心
药物安全性评价中心
通讯作者He, Hai-Bing
作者单位1.E China Normal Univ, Inst Med Chem, Shanghai 200062, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China;
3.E China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China;
4.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China
推荐引用方式
GB/T 7714		 He, Hai-Bing,Gao, Li-Xin,Zhou, Yue-Yang,et al. DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2,5-DIPHENYL-1,3,4-OXADIAZOLE DERIVATIVES AS NOVEL INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE[J]. HETEROCYCLES,2012,85(11):2693-2712.
APA He, Hai-Bing.,Gao, Li-Xin.,Zhou, Yue-Yang.,Liu, Ting.,Tang, Jie.,...&Yang, Fan.(2012).DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2,5-DIPHENYL-1,3,4-OXADIAZOLE DERIVATIVES AS NOVEL INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE.HETEROCYCLES,85(11),2693-2712.
MLA He, Hai-Bing,et al."DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2,5-DIPHENYL-1,3,4-OXADIAZOLE DERIVATIVES AS NOVEL INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE".HETEROCYCLES 85.11(2012):2693-2712.

入库方式： OAI收割

来源：上海药物研究所

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