吡唑并三嗪酮类化合物的合成及生物活性测定
Synthesis and Bioassay of Pyrazolotriazinones
摘要
为了发现新型的原卟啉原氧化酶抑制剂，根据生物合理设计方法，设计并合成了一系列结构新颖的3H-吡唑并[3,4-d][1,2,3]三嗪-4-酮衍生物。利用不同取代的5-氨基-吡唑-4-甲酰氯与取代苯胺反应制得的5-氨基-N-苯基-1H-吡唑-4-甲酰胺衍生物，经进一步重氮化得到目标化合物，并对化合物3f进行衍生化。所得目标化合物的结构均经1H NMR和元素分析确证。其中，化合物3d的结构还经过单晶确定。生物活性测定结果表明，部分化合物对原卟啉原氧化酶有较高的抑制活性，讨论了结构与活性的关系。
Abstract
In order to find new protoporphyrinogen oxidase inhibitors, a series of novel 3H-pyrazolo[3,4-d][1,2,3]triazin-4-one derivatives were designed and synthesized according to biorational design. The target molecules were synthesized by diazotization of different 5-amino-N-phenyl-1H-pyrazole-4-carboxamide derivatives prepared by a reaction of substituted 5-amino-pyrazole-4-carbonyl chloride with substituted anilines. Different halides were reacted with 3f to afford the pure target products 3g~3n respectively. Their structures were identified by 1H NMR and elemental analyses. The structure of 3d was further confirmed by X-ray single crystal diffraction. The bioassay results showed that some of the title compounds exhibited good inhibition against protoporphyrinogen oxidase activity in vitro. The structure-activity relationship was discussed.关键词
植物保护/吡唑并三嗪酮/原卟啉原氧化酶/生物活性Key words
plant protection/pyrazolotriazinone/protoporphyrinogen oxidase/bioactivity引用本文复制引用
杨华铮,李华斌.吡唑并三嗪酮类化合物的合成及生物活性测定[EB/OL].(2013-02-04)[2025-12-27].http://www.paper.edu.cn/releasepaper/content/201302-37.学科分类
药学/生物化学/农药工业
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