中文题名: | 靶向 CSF-1受体的邻氨基吡啶炔基类分子探针的设计和合成 |
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保密级别: | 公开 |
论文语种: | 中文 |
学科代码: | 070301 |
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学生类型: | 学士 |
学位: | 理学学士 |
学位年度: | 2022 |
学校: | 北京师范大学 |
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第一导师姓名: | |
第一导师单位: | |
第二导师姓名: | |
提交日期: | 2022-06-01 |
答辩日期: | 2022-05-18 |
外文题名: | Design and synthesis of an o-aminopyridine alkynyl molecular probe targeting the CSF-1 receptor |
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外文关键词: | |
中文摘要: |
利用邻氨基吡啶炔基类化合物1作为先导化合物,设计了一种新的18F标记的CSF-1受体分子探针,合成了其稳定化合物2,并采用核磁共振氢谱(1H NMR)、氟谱(19F NMR)以及质谱(MS)对中间体和目标产物的结构进行了分析鉴定。结果表明,合成的最终产物与设计的目标化合物结构一致。测定了目标化合物2对CSF-1受体激酶活性抑制的IC50值,发现化合物2的激酶活性抑制能力明显低于化合物1,说明在邻氨基吡啶炔基类化合物的苯环对位引入大的取代基会降低化合物对CSF-1受体激酶活性的抑制能力。本文结果为进一步设计性质优异的CSF-1受体分子探针提供了参考。 |
外文摘要: |
Using o-aminopyridine alkynyl compound 1 as lead compound, a 18F-labeled molecular probe targeting the CSF-1 receptor was designed. The reference compound (2) was synthesized. The structures of the intermediates and the target compound were analyzed and validated by 1H NMR, 19F NMR and mass spectrometry (MS). In vitro kinase enzyme assay was performed. The results showed the decreased inhibitory activity of compound 2 against the CSF-1 receptor compared to that of compound 1, indicating introduction of large substituent at the para-position of the benzene ring decreased the inhibitory activity of the o-aminopyridine alkynyl compounds. The results are useful for further structural modifications to explore new potential radiotracers for the CSF-1 receptor. |
参考文献总数: | 33 |
作者简介: | 罗皓 |
插图总数: | 26 |
插表总数: | 4 |
馆藏号: | 本070301/22057 |
开放日期: | 2023-06-01 |