Parallel synthesis of oligonucleotides containing N-acyl amino-LNA and their therapeutic effects as anti-microRNAs

Abstract

2′-Amino-locked nucleic acid (ALNA), maintains excellent duplex stability, and the nitrogen at the 2′-position is an attractive scaffold for functionalization. Herein, a facile and efficient method for the synthesis of various 2′-N-acyl amino-LNA derivatives by direct acylation of the 2′-amino moiety contained in the synthesized oligonucleotides and its fundamental properties are described. The introduction of the acylated amino-LNA enhances the potency of the molecules as therapeutic anti-microRNA oligonucleotides.