Chimie Thérapeutique, Université Paris Descartes, CNRS UMR 8638, 4 avenue de l'Observatoire, 75006, Paris, France.
Org Biomol Chem. 2010 Mar 7;8(5):1154-9. doi: 10.1039/b921232a. Epub 2010 Jan 19.
A small library of 1,5-triazole derivatives linking a diaminocyclopentadiol and aromatic ketones has been prepared and screened using NMR and fluorescent techniques against tRNA(Lys)(3), the HIV reverse transcription primer. The comparison of their binding properties to those of their 1,4-triazole isomers, previously discovered in a fragment-based approach, outlines the influence of the linker on affinity and binding selectivity in such an approach.
已经制备并使用 NMR 和荧光技术筛选了一个连接二氨基环戊二烯和芳香酮的 1,5-三唑衍生物的小文库，针对 tRNA(Lys)(3)（HIV 逆转录引物）。与以前基于片段的方法中发现的 1,4-三唑异构体相比，比较它们的结合性质，概述了这种方法中连接子对亲和力和结合选择性的影响。
