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Synthesis and structure-activity relationship of non-phosphorus-based fructose-1,6-bisphosphatase inhibitors: 2,5-Diphenyl-1,3,4-oxadiazoles

文献类型：期刊论文

作者Liao, Ben-Ren3; He, Hai-Bing2,3; Yang, Ling-Ling1; Gao, Li-Xin1; Chang, Liang3; Tang, Jie3; Li, Jing-Ya1; Li, Jia1; Yang, Fan3
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2014-08-18
卷号83页码:15-25
关键词Diabetes Antidiabetic Fructose-1,6-bisphosphatase (FBPase) Inhibitor 2,5-Diphenyl-1,3,4-oxadiazoles
ISSN号0223-5234
DOI10.1016/j.ejmech.2014.06.011
文献子类Article
英文摘要With the aim of discovering a novel class of non-phosphorus-based fructose-1,6-bisphosphatase (FBPase) inhibitors, a series of 2,5-diphenyl-1,3,4-oxadiazoles were synthesized based on the hit compound (1) resulting from a high-throughput screening (HTS). Structure-activity relationship (SAR) studies led to the identification of several compounds with comparable inhibitory activities to AMP, the natural allosteric inhibitor of FBPase. Notably, compound 22 and 27b, bearing a terminal carboxyl or 1H-tetrazole, demonstrated remarkable inhibition to gluconeogenesis (GNG). In addition, both inhibition and binding mode to the enzyme were investigated by enzymatic kinetics and in silico experiments for representative compounds 16 and 22. (C) 2014 Published by Elsevier Masson SAS.
WOS关键词HEPATIC GLUCOSE-PRODUCTION ; DEPENDENT DIABETES-MELLITUS ; FRUCTOSE 1,6-BISPHOSPHATASE ; BENZOXAZOLE BENZENESULFONAMIDES ; ALLOSTERIC INHIBITORS ; DEVELOPMENT SETTINGS ; ESTIMATE SOLUBILITY ; DRUG DISCOVERY ; GLUCONEOGENESIS ; AMP
资助项目Shanghai Science and Technology Council[12142200800] ; Shanghai Science and Technology Council[13142200900] ; Shanghai Science and Technology Council[13DZ2290300] ; 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[2013ZX09507002] ; National Science Fund for Distinguished Young Scholars[81125023] ; Laboratory of Organic Functional Molecules, Sino-French Institute of ECNU[00000000]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000340689600002
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/276938]  
专题国家新药筛选中心
药物安全性评价中心
通讯作者Li, Jia
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 207203, Peoples R China;
2.Nantong Univ, Nantong 226019, Jiangsu, Peoples R China
3.E China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Dept Chem, Shanghai 200062, Peoples R China;
推荐引用方式
GB/T 7714		 Liao, Ben-Ren,He, Hai-Bing,Yang, Ling-Ling,et al. Synthesis and structure-activity relationship of non-phosphorus-based fructose-1,6-bisphosphatase inhibitors: 2,5-Diphenyl-1,3,4-oxadiazoles[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,83:15-25.
APA Liao, Ben-Ren.,He, Hai-Bing.,Yang, Ling-Ling.,Gao, Li-Xin.,Chang, Liang.,...&Yang, Fan.(2014).Synthesis and structure-activity relationship of non-phosphorus-based fructose-1,6-bisphosphatase inhibitors: 2,5-Diphenyl-1,3,4-oxadiazoles.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,83,15-25.
MLA Liao, Ben-Ren,et al."Synthesis and structure-activity relationship of non-phosphorus-based fructose-1,6-bisphosphatase inhibitors: 2,5-Diphenyl-1,3,4-oxadiazoles".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 83(2014):15-25.

入库方式： OAI收割

来源：上海药物研究所

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