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一些吲哚二酮类衍生物的合成及对AHAS的抑制活性
  • 期刊名称：高等学校化学学报
  • 时间：0
  • 页码：192503-1-192503-3
  • 语言：中文
  • 分类：O626[理学—有机化学;理学—化学]
  • 作者机构：[1]南开大学元素有机化学研究所,元素有机化学国家重点实验室,天津300071
  • 相关基金：国家自然科学重点基金（批准号：20432010）和国家自然科学青年基金（批准号：20602021）资助.
  • 相关项目：基于靶酶结构设计新型AHAS抑制剂
作者： 谭海忠|李慧东|李永红|王建国|李正名|李文明|
关键词： 新型AHAS抑制剂, 吲哚二酮类化合物, 生物活性, Novel AHAS inhibitor, Isatin derivatives, Biological activity
中文摘要：

基于一些新结构特征的AHAS抑制剂，设计并合成了一系列吲哚二酮类化合物．初步的生物活性测试结果表明，所合成的化合物在体内和体外均具有一定的生物活性，其中，化合物13在100μg/mL浓度下对AHAS的抑制达到85％，化合物7（平皿法）在100μg/mL浓度条件下对油菜胚根生长抑制率可达84．7％，是一类未见文献报道的结构新型的AHAS抑制剂，有望为进一步设计合成更高活性的化合物提供参考．

英文摘要：

Based on the crystal structure of AHAS enzyme, bio-rational drug design was used to discover some novel AHAS inhibitors via computational virtual screening. Some isatin derivatives as AHAS inhibitors were designed, synthesized and evaluated. The preliminary results show that the isatin compounds exhibit conside- rate inhibition both in vivo and in vitro against AHAS. Compound 13 show an inhibition of 85% at 100μg/mL concentration in vitro and compound 7 show an inhibition of 84.7% of rape root length at 100 μg/mL concen-tration. This discovery provides meaningful information for further design and synthesis of novel compounds with enhanced activity.

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