Synthesis and Biophysical Properties of Phosphorodiamidate Piperidino Oligomers

Org Lett. 2023 Feb 17;25(6):901-906. doi: 10.1021/acs.orglett.2c04067. Epub 2023 Feb 3.

Abstract

We report the synthesis of piperidino nucleoside phosphoramidates functionalized with uracil, cytosine, guanine, and adenine and their incorporation into oligomers. High-performance liquid chromatography analyses demonstrated that a phosphorodiamidate piperidino oligomer (PPO) is more lipophilic than a phosphorodiamidate morpholino oligomer (PMO) of the same tetrameric sequence. A PMO containing piperidino residues formed duplexes with both DNA and RNA, and the PPO had higher stability at endosomolytic pH and higher hydrophobicity than the PMO.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Morpholinos
  • Oligonucleotides, Antisense*

Substances

  • Oligonucleotides, Antisense
  • Morpholinos