中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
synthesisandproteintyrosinephosphatase1binhibitoryactivityevaluationofindolepropylbased134oxadiazolederivatives

文献类型:期刊论文

作者Mei WW(梅雯雯)1; Guo YW(郭跃伟)2; Li J(李佳)2; Cai MY(蔡妹艺)1; Ma WQ(马文泉)3; Gong JX(龚景旭)2; Wang XD(王学东)1
刊名chinesejournaloforganicchemistry
出版日期2016
卷号36期号:3页码:533
关键词MARINE NATURAL-PRODUCTS BIOLOGICAL EVALUATION LYCOGARUBIN C PHIDIANIDINES PROGRESS DESIGN DRUGS 1,3,4-oxadiazole synthesis PTP1B inhibitory activity
ISSN号0253-2786
DOI10.6023/cjoc201509024
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.
资助项目[National Marine "863" Projects] ; [National Natural Science Foundation of China] ; [NSFC-Shandong Joint Fund for Marine Science Research Centers] ; [Science and Technology Commission of Shanghai Municipality Project] ; [State Key Laboratory of Drug Research/Shanghai Institute of Materia Medica Projects]
语种英语
源URL[http://119.78.100.183/handle/2S10ELR8/284846]  
专题中国科学院上海药物研究所
作者单位1.潍坊医学院
2.中国科学院上海药物研究所
3.潍坊生物医药创新创业服务中心
推荐引用方式
GB/T 7714
Mei WW,Guo YW,Li J,et al. synthesisandproteintyrosinephosphatase1binhibitoryactivityevaluationofindolepropylbased134oxadiazolederivatives[J]. chinesejournaloforganicchemistry,2016,36(3):533.
APA 梅雯雯.,郭跃伟.,李佳.,蔡妹艺.,马文泉.,...&王学东.(2016).synthesisandproteintyrosinephosphatase1binhibitoryactivityevaluationofindolepropylbased134oxadiazolederivatives.chinesejournaloforganicchemistry,36(3),533.
MLA 梅雯雯,et al."synthesisandproteintyrosinephosphatase1binhibitoryactivityevaluationofindolepropylbased134oxadiazolederivatives".chinesejournaloforganicchemistry 36.3(2016):533.

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来源:上海药物研究所

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