Oligonucleotides containing n-methyl thiolated bases having anti

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

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C07H 2102, A61K 3170

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active

056523599

ABSTRACT:
Oligonucleotides containing 1-N-alkyl-6-thiopurine, 3-N-alkyl-4-thiopyrimidine and 5-N-alkyl-4-thiopyrazolopyrimidine bases and the corresponding 2'-O-alkylated or allylated nucleotides demonstrate potent antiviral activity in several assays, including the human immunodeficiency virus reverse transcriptase enzyme assay. The oligonucleotides of the invention contain approximately 5 to 99 nucleotide units, and may include, in addition to the above-noted N-alkylated and thiolated heterocyclic bases, the naturally occurring pyrimidine and purine bases.

REFERENCES:
patent: 5416203 (1995-05-01), Lestinger
Chan et al. J. Gen. Virol. 52:241-249, 1981, month not available.
Amarnath et al. Biochimica et Biophysica Acta 474:16-23 (1977), month not available.
Amarnath et al. Biochemistry 15(20):4386-4389, 1976, month not available.
Iribarren et al. Proc. Natl. Acad. Sci. 87:7747-7751, 1990.
Broom A. D. et al., "Synthesis and PMR Studies of some Methylated 6-Thiopurine Nucleosides (1)", J. Heterocyclic Chem. 12, 171-174 (1975), month not available.
Saamu Shibahara et al., "Inhibition of human immunodeficiency virus (HIV-1) replication by synthetic oligo-RNA", Nucleic Acid Research, vol. 17, No. 1, pp. 239-252 (1989), month not available.

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