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Summary
Novelty: The synthesis of novel oligonucleotides which contain nitrogenous moieties, such as polyamines or hydrazines, is disclosed. These polyamine conjugated phosphonothioate oligonucleotides may be useful in antisense therapy and are claimed to enhance cellular uptake nuclease resistance and to target the tat region of HIV, thereby making them potential anti-HIV agents.
Biology: No biological data are presented.
Chemistry: The three-step synthesis of 1,3-diphenylimidazoline protected 5′-aldehydic-3′-(2-cyanoethyl-N,N-diisopropylphophoramidityl)thymidine and its subsequent elaboration to the target oligonucleotides is described. Seven examples are included.
Structure: 