吲哚丙基-1,3,4-噁二唑衍生物的合成及蛋白酪氨酸磷酸酯酶1B抑制活性研究
收稿日期: 2015-09-21
修回日期: 2015-11-12
网络出版日期: 2015-12-04
基金资助
国家海洋"863"项目(Nos. 2013AA092902, 2012AA092105)、国家自然科学基金(Nos. 81520108028, 81273430, 41306130, 41506187, 81302692, 41476063)、山东省自然科学基金(No. U1406402)、上海市科委项目(Nos. 14431901100, 15431901000)、新药研究国家重点实验室/上海药物所自主项目(Nos. SIMM1501ZZ-03, CASIMM0120152039)资助项目.
Synthesis and Protein-Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Indolepropyl Based 1,3,4-Oxadiazole Derivatives
Received date: 2015-09-21
Revised date: 2015-11-12
Online published: 2015-12-04
Supported by
Project supported by the National Marine "863" Projects (Nos. 2013AA092902 and 2012AA092105), the National Natural Science Foundation of China (Nos. 81520108028, 81273430, 41306130, 41506187, 81302692, 41476063), the NSFC-Shandong Joint Fund for Marine Science Research Centers (No. U1406402), the Science and Technology Commission of Shanghai Municipality Project (Nos. 14431901100, 15431901000), the State Key Laboratory of Drug Research/Shanghai Institute of Materia Medica Projects (Nos. SIMM1501ZZ-03, CASIMM0120152039).
梅雯雯 , 郭跃伟 , 李佳 , 蔡妹艺 , 马文泉 , 龚景旭 , 王学东 . 吲哚丙基-1,3,4-噁二唑衍生物的合成及蛋白酪氨酸磷酸酯酶1B抑制活性研究[J]. 有机化学, 2016 , 36(3) : 533 -539 . DOI: 10.6023/cjoc201509024
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 μg· mL-1 . It was the first example of indolealkyl based oxadiazole derivatives showing PTP1B inhibitory activity.
Key words： 1,3,4-oxadiazole; synthesis; PTP1B inhibitory activity
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