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肉芝软珊瑚属中二聚西松烷型二萜化合物的化学和生物活性研究进展
  • ISSN号：0253-2786
  • 期刊名称：有机化学
  • 时间：2013.6.6
  • 页码：1157-1166
  • 分类：TQ457.29[化学工程—农药化工]
  • 作者机构：[1]潍坊医学院药学院,潍坊261053, [2]中国科学院上海药物研究所新药研究国家重点实验室,上海201203, [3]潍坊生物医药创新创业服务中心,潍坊261205
  • 相关基金：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~~
  • 相关项目：三种南海软珊瑚的化学成分分离、结构鉴定及其生物活性研究
作者： 李玉芬|梁林富|萧伟|梁敬钰|郭跃伟|
关键词： 1, 3, 4-噁二唑, 合成, PTP1B抑制活性, 1, 3, 4-oxadiazole, synthesis, PTP1B inhibitory activity
中文摘要：

以吲哚丁酸为原料,通过酯化、酰肼化、环化、取代四步反应得到了一系列吲哚丙基-1,3,4-噁二唑衍生物.对所合成的目标化合物进行了抗蛋白酪氨酸磷酸酯酶1B（PTP1B）活性测试,发现其中5个化合物具有明显的体外抗PTP1B活性,其中化合物5g活性最强,其IC_（50）为6.74μg·mL^-1.该系列化合物是首次报道的具有PTP1B抑制活性的吲哚烷基-噁二唑衍生物.

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 PTP1 B in vitro, for instance, compound 5g exhibited the strongest PTP1 B inhibitory activity with an IC_（50） value of 6.74 μg·m L~（-1）. It was the first example of indolealkyl based oxadiazole derivatives showing PTP1 B inhibitory activity.

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三种南海软珊瑚的化学成分分离、结构鉴定及其生物活性研究
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期刊信息
  • 《有机化学》
  • 中国科技核心期刊
  • 主管单位:
  • 主办单位:中国化学会 中国科学院上海有机化学研究所
  • 主编：陈庆云
  • 地址：上海市枫林路354号
  • 邮编：200032
  • 邮箱：bianji@mail.sioc.ac.cn
  • 电话：021-54925244
  • 国际标准刊号：ISSN：0253-2786
  • 国内统一刊号：ISSN：31-1321/O6
  • 邮发代号:4-285
  • 获奖情况:
  • 中国期刊方阵“双效”期刊
  • 国内外数据库收录:
  • 俄罗斯文摘杂志,美国化学文摘（网络版）,荷兰文摘与引文数据库,美国科学引文索引（扩展库）,日本日本科学技术振兴机构数据库,中国中国科技核心期刊,中国北大核心期刊（2004版）,中国北大核心期刊（2008版）,中国北大核心期刊（2011版）,中国北大核心期刊（2014版）,中国北大核心期刊（2000版）
  • 被引量:14408