顺序 DNA 编码砌块融合用于构建多取代吡唑啉核心库。
Sequential DNA-Encoded Building Block Fusion for the Construction of Polysubstituted Pyrazoline Core Libraries.
机构信息
Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, Chongqing 401331, P. R. China.
Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing, 400044, P. R. China.
出版信息
Org Lett. 2021 Nov 5;23(21):8429-8433. doi: 10.1021/acs.orglett.1c03145. Epub 2021 Oct 15.
The construction of chemical libraries containing polysubstituted pyrazoline scaffolds is highly desirable for the discovery of novel chemical ligands for biological targets. Herein, we report a sequential DNA-encoded synthesis strategy for polysubstituted pyrazoline heterocycles, which fuses a broad panel of aldehydes, aryl amines, and alkenes as building blocks. Furthermore, mock library synthesis and selection demonstrated the ability of the method to produce DNA-encoded focused libraries with highly functionalized pyrazoline cores.
构建含有多取代吡唑啉骨架的化学文库对于发现新型生物靶标化学配体具有重要意义。本文报道了一种序列 DNA 编码合成多取代吡唑啉杂环的方法，该方法融合了广泛的醛、芳基胺和烯烃作为构建块。此外，模拟文库合成和选择证明了该方法能够产生具有高度功能化吡唑啉核心的 DNA 编码聚焦文库。
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