Design And Synthesis Of An Azabicyclic Nucleoside Phosphoramidite For Oligonucleotide Antisense Constructs.

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.
PMID: 31380707 [PubMed - as supplied by publisher]

Source: Nucleosides, Nucleotides and Nucleic Acids - August 7, 2019 Category: Biochemistry Tags: Nucleosides Nucleotides Nucleic Acids Source Type: research