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查尔酮类化合物的设计与合成

Design and Synthesis of Chalcone Compounds

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【作者】 王杰李波张晖张恩立汤泉

【Author】 WANG Jie;LI Bo;ZHANG Hui;ZHANG En-li;TANG Quan;Public Basic College, Bengbu Medical College;

【机构】 蚌埠医学院公共基础学院

【摘要】 设计、合成可能具有抗血小板聚集活性的查尔酮类化合物,为抗血小板聚集候选药物的开发提供参考。以(E)-查耳酮为模型化合物,依据药物化学中的分子片段理论,设计含有羟基的查尔酮类化合物。以取代苯甲醛或川芎嗪醛、丹皮酚或对羟基苯乙酮为起始原料,通过氧化反应、酯化反应、水解反应、羟醛缩合反应等步骤对设计的化合物进行合成。采用1H NMR、13C NMR、MS技术手段对合成的化合物结构进行表征。实验设计、合成了9个查尔酮类化合物,丰富了该类化合物的结构库,为抗血小板聚集药物开发提供参考。

【Abstract】 This paper is to design and synthesize chalcone compounds with anti-platelet aggregation activity. The chalcone compounds provide a reference for the development of candidate drugs for anti platelet aggregation. According to the molecular fragment theory in pharmaceutical chemistryusing, chalcone compounds containing hydroxyl groups were designed based on(E)-chalcone as the model compound. Designed compounds were synthesized by oxidation reaction, esterification reaction, hydrolysis reaction and aldol condensation reaction. Their starting materials were substituted benzaldehyde or Ligustrazine aldehyde, paeonol or p-hydroxyacetophenone. The structures of the synthesized compounds were characterized by 1H NMR, 13C NMR and MS. Nine chalcone compounds were designed and synthesized, which enriched the structural library of chalcone compounds and provided a reference for the development of antiplatelet aggregation drugs.

【关键词】 查尔酮设计合成
【Key words】 chalconedesignsynthesis
【基金】 蚌埠医学院自然科学基金重点项目“丹皮酚衍生物的设计、合成及抗血小板聚集活性研究”(BYKY1824ZD);安徽省高校自然科学研究项目“新型四氢异喹啉靶向抗肿瘤药物的设计、合成及活性筛选”(KJ2019A0390)
  • 【文献出处】 长春师范大学学报 ,Journal of Changchun Normal University , 编辑部邮箱 ,2021年10期
  • 【分类号】TQ460.6
  • 【下载频次】778
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