Oligonucleotide dimers with amide linkages replacing phosphodies

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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536 243, 536 256, C07H 1900, C07H 2100, C07H 2102, C07H 2104

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056633122

ABSTRACT:
Disclosed are oligonucleotide analogs comprising oligonucleoside sequences having from 3 to about 200 bases and containing internucleoside linkages wherein amide linkages replace phosphodiester linkages that are the backbones of the natural oligonucleotides that make up RNA and DNA. Also disclosed are bifunctional nucleoside analogs, a process for preparing dimers and trimers therefrom, and a method of using these bifunctional nucleoside intermediates, including the dimers and trimers, to synthesize the above-described oligonucleotide analogs using conventional synthetic organic procedures known in the art, preferably in a solid phase synthesis, more preferably in an automated peptide synthesizer.

REFERENCES:
Gura "Antisense has growing pains" Science 270:575-577 Oct. 27, 1995.
Milligan et al. "Current concepts in Antisense drug design" J. Medicinal Chem. 36(14):1923-1927 Jul. 9, 1993.

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