- Modified nucleosides for the treatment of viral infections and abnormal cellular proliferation
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The disclosed invention is a composition for and a method of treating a Flaviviridae (including BVDV and HCV), Orthomyxoviridae (including Influenza A and B) or Paramyxoviridae (including RSV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans, using a nucleoside of general formula (I)-(XXIII) or its pharmaceutically acceptable salt or prodrug. This invention also provides an effective process to quantify the viral load, and in particular BVDV, HCV or West Nile Virus load, in a host, using real-time polymerase chain reaction (""RT-PCR""). Additionally, the invention discloses probe molecules that can fluoresce proportionally to the amount of virus present in a sample.
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- Process for the deoxygenation of nucleosides
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An efficient process for the deoxygenation of 2'- and or 3'-hydroxyl groups of a nucleoside that includes reacting the hydroxyl group with 3-halopropionitrile or 2-nitroethylhalide and carbon disulfide in base to form a 2'- or 3'-(cyanoethylthio or nitroethylthio)thiocarbonyl, that is reductively eliminated and replaced with hydrogen. The deoxygenation process can be used in a wide variety of nucleoside syntheses that require the elimination of the 2'- or 3'-hydroxyl groups, including the preparation of 3'-substituted-2',3'-dideoxynucleosides such as 3'-azido-3'-deoxythymidine and 3'-azido-2',3'-dideoxyuridine.
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- Discovery of a Novel Route to β-Thymidine: a Precursor for anti-AIDS Compounds
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A new approach to the synthesis of β-thymidine from D-xylose is described.
- Rao, A. V. Rama,Gurjar, Mukund K.,Lalitha, Sista V. S.
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p. 1255 - 1256
(2007/10/02)
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- Synthesis of β-D-xylofuranosyl- and 2,2'-anhydro-1-β-D-lyxofuranosylpyrimidine nucleosides
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β-D-Xylofuranosylpyrimidines were obtained by condensation of silyl derivatives of pyrimidines with 1,2-di-O-acetyl-3,5-di-O-benzoyl-D-xylofuranose with subsequent deprotection of the sugar fragment.Refluxing 2-O-tosyl derivatives of nucleosides with NaI
- Tolstikov, G.A.,Mustafin, A.G.,Gataullin, R.R.,Spirikhin, L.V.,Sultanova, V.S.,Abdrakhmanov, I.B.
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p. 1095 - 1099
(2007/10/02)
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- 1-(β-D-xylofuranosyl)thymine derivatives
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This invention relates to a new synthetic process for the manufacture of zidovudine from the starting material D-xylose involving: (i) Conversion of D-xylose to a 1-(β-D-xylofuranosyl)thymine derivative; (ii) 2'-Deoxygenation of the thymine derivative; and (iii) 3'-Azidation of the 2'-deoxy compound.
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- Chemical process
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This invention relates to a new synthetic process for the manufacture of zidovudine from the starting material D-xylose involving: i) Conversion of D-xylose to a 1-(β-D-xylofuranosyl)thymine derivative; ii) 2?-Deoxygenation of the thymine derivative; and iii) 3?-Azidation of the 2?-deoxy compound.
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- Process for the preparation of 3'-azido-3'-deoxythymidine and intermediates
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This invention relates to a new synthetic process for the manufacture of zidovudine from the starting material D-xylose involving: i) Conversion of D-xylose to a 2′,3′,5′-protected derivative of 1-(β-D-xylofuranosyl)thymine; ii) 2′-Deoxygenation of the xylofuranosyl thymine; and iii) 3′-Azidation of the 2′-deoxy compound.
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- Systematic Synthesis and Biological Evaluation of α- and β-D-Xylofuranosyl Nucleosides of the Five Naturally Occurring Bases in Nucleic Acids and Related Analogues
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The α- and β-D-xylofuranosyl analogues of the naturally occurring nucleosides, as well as other D-xylofuranosyl derivatives, have been the subject of a systematic synthesis and examination of their biological, i.e. antiviral antimetabolic, and cytostatic
- Gosselin, Gilles,Bergogne, Marie-Chistine,Rudder, Jean de,Clercq, Erik De,Imbach, Jean-Louis
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p. 203 - 213
(2007/10/02)
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