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Synthesis and Protein-Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Indolepropyl Based 1,3,4-Oxadiazole Derivatives

文献类型：期刊论文

作者Mei Wenweeb2,3; Guo Yuewei3; Li Jia3; Cai Meiyi2; Ma Wenquan1; Gong Jingxu3; Wang Xuedong2
刊名CHINESE JOURNAL OF ORGANIC CHEMISTRY
出版日期2016-03
卷号36期号:3页码:533-539
关键词1,3,4-oxadiazole synthesis PTP1B inhibitory activity
ISSN号0253-2786
DOI10.6023/cjoc201509024
文献子类Article
英文摘要A series of indolepropyl based 1,3,4-oxadiazole derivatives were synthesized by esterification, hydrazidation, cyclization and substitution using indolebutyric acid as starting material. The inhibitory activity against protein tyrosine phosphatase 1B (PTP1B) was evaluated. The results indicated that five compounds displayed obviously inhibitory effect against PTP1B in vitro, for instance, compound 5g exhibited the strongest PTP1B inhibitory activity with an IC50 value of 6.74 mu g.mL(-1). It was the first example of indolealkyl based oxadiazole derivatives showing PTP1B inhibitory activity.
WOS关键词MARINE NATURAL-PRODUCTS ; BIOLOGICAL EVALUATION ; LYCOGALIC ACID ; LYCOGARUBIN C ; PHIDIANIDINES ; PROGRESS
资助项目National Marine "863" Projects[2013AA092902] ; National Marine "863" Projects[2012AA092105] ; National Natural Science Foundation of China[81520108028] ; National Natural Science Foundation of China[81273430] ; National Natural Science Foundation of China[41306130] ; National Natural Science Foundation of China[41506187] ; National Natural Science Foundation of China[81302692] ; National Natural Science Foundation of China[41476063] ; NSFC-Shandong Joint Fund for Marine Science Research Centers[U1406402] ; Science and Technology Commission of Shanghai Municipality Project[14431901100] ; Science and Technology Commission of Shanghai Municipality Project[15431901000] ; State Key Laboratory of Drug Research/Shanghai Institute of Materia Medica Projects[SIMM1501ZZ-03] ; State Key Laboratory of Drug Research/Shanghai Institute of Materia Medica Projects[CASIMM0120152039]
WOS研究方向Chemistry
语种中文
CSCD记录号CSCD:5684276
WOS记录号WOS:000375637600010
出版者SCIENCE PRESS
源URL[http://119.78.100.183/handle/2S10ELR8/276109]  
专题天然药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Gong Jingxu; Wang Xuedong
作者单位1.Weifang Biomed Innovat & Entrepreneurship Serv, Weifang 261205, Peoples R China
2.Weifang Med Univ, Coll Pharm, Weifang 261053, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Mei Wenweeb,Guo Yuewei,Li Jia,et al. Synthesis and Protein-Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Indolepropyl Based 1,3,4-Oxadiazole Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2016,36(3):533-539.
APA Mei Wenweeb.,Guo Yuewei.,Li Jia.,Cai Meiyi.,Ma Wenquan.,...&Wang Xuedong.(2016).Synthesis and Protein-Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Indolepropyl Based 1,3,4-Oxadiazole Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,36(3),533-539.
MLA Mei Wenweeb,et al."Synthesis and Protein-Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Indolepropyl Based 1,3,4-Oxadiazole Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 36.3(2016):533-539.

入库方式： OAI收割

来源：上海药物研究所

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