Abstract We report the synthesis and biophysical evaluation of an azabicycle dinucleotide with restricted γ, β, and ε torsion angles, featuring the introduction of a piperidine ring that locks the conformation of the nucleoside into an RNA-type nucleic acid. The conceptual basis of the design is predicated upon the notion that the conformation of the phosphate group linking two RNA nucleotides can be approximated with an azabicyclic phosphoramidite which may also benefit from a unique stereoelectronic effect. Graphical Abstract

中文翻译：

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用于寡核苷酸反义构建体的氮杂双环核苷亚磷酰胺的设计与合成

摘要 我们报告了具有受限 γ、β 和 ε 扭转角的氮杂双环二核苷酸的合成和生物物理评估，其特征是引入了哌啶环，将核苷的构象锁定为 RNA 型核酸。该设计的概念基础基于这样一个概念，即连接两个 RNA 核苷酸的磷酸基团的构象可以近似为氮杂双环亚磷酰胺，这也可能受益于独特的立体电子效应。图形概要