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光C-C结合的triazole-Purine结合物的合成

Aleksejs Burcevs¹, Armands Sebris¹, Kaspars Traskovskis²

¹Institute of Technology of Organic Chemistry, Faculty of Materials Science and Applied Chemistry, Riga Technical University, P. Valdena Str. 3, Riga, LV-1048, Latvia.

Journal of fluorescence

|July 17, 2023

概括

新的三醇-纯氨酸合物被合成,具有出色的光特性和低细胞毒性. 这些化合物由于其独特的特性和生物兼容性,具有各种应用的潜力.

科学领域:

有机化学有机化学
材料科学材料科学材料科学
药用化学医学化学

背景情况:

纯氨酸衍生物是药物化学中的关键支架.
三醇部分增强分子性质和生物活性.
光有机分子对于成像和传感应用至关重要.

研究的目的:

为了合成新型的C-C结合的2,6-bis(1H-1,2,3-triazol-4-yl) -9H-纯氨酸和2-piperidinyl-6-(1H-1,2,3-triazol-4-yl) -9H-纯氨酸衍生物.
为了研究这些三醇-纯氨酸合物的光特性.
为了评估合成化合物的细胞毒性.

主要方法:

使用了三,索诺加希拉,铜 (I) 催化亚酸环添加和S_NAr反应的组合.
合成了11个2,6-bistriazolylpurine的例子和14个2-piperidinyl-6-triazolylpurine中间体的例子.
在溶液和薄膜中研究光特性.

主要成果:

获得的产量为bistriazolylpurines的38-86%和monotriazolylpurines的41-89%.
观察到显著的光性质,量子产量高达49% (bistriazolylpurines) 和95% (monotriazolylpurines) 的光性质.
在小鼠胚胎纤维细胞体,人类角质细胞和小鼠前列腺细胞系中表现出低细胞毒性,IC₅₀值从59.6到1528.7μM.

结论:

成功设计和合成了具有C-C键的新型三醇-纯氨酸结合物.
合成的化合物表现出有希望的光特性.
大多数衍生品表现出良好的安全性,表明进一步开发的潜力.

关键词:

这就是CuAACAC.光是一种光效应.光纯素是一种光纯素.索诺加希拉的反应

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