By C.K. Chu
• updated overview at the chemistry and biology of nucleosides • smooth man made method • complete assurance of antiviral nucleosidesThis booklet summarizes the hot advances in nucleosides chemistry and chemotherapy during the last 10-15 years. It covers lately chanced on nucleoside antiviral brokers, their healing facets and biochemistry, and in addition large experiences on their chiral synthesis.
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Extra resources for Antiviral Nucleosides: Chiral Synthesis and Chemotherapy
Choi and C. K. Chu 2',3'-Unsaturated nucleosides and related analog Although for nucleoside analogs it has not been possible to elaborate a pharmacophore, 2',3'-unsaturated sugars are probably the most effective moieties for the inhibition of HIV and HBV replication. Among compounds with this feature, 2',3'-didehydro-2',3'dideoxythymidine (83, d4T, stavudine)^'* and its carbocyclic 2-amino-6-cyclopropylaminopurine analog (84, 1592U89, abacavir)^^ have been approved for the treatment of HIV infection (Figure 30).
1995, 39, 979-981. 13. (a) Prusoff, W. H. Synthesis and biological activities of iododeoxyuridine, an analog of thymidine. Biochim. Biophys. Acta 1959, 32, 295-296. (b) Kaufman, H. ; Heidelberger, C. Therapeutic antiviral action of 5-trifluoromethyl-2-deoxyuridine in herpes simplex keratitis. Science 1964, 745, 585-586. (c) De Clercq, E. Synthetic pyrimidine nucleoside analogs. In Approaches to Antiviral Agents, Hamden, M. ; Macmillan: London, 1985, pp. 57-99. (d) De Clercq, E. : London, 1988, Vol.
Earl, R. A. Synthesis of carbocyclic nucleosides. Tetrahedron 1994, 50, 10611-10670. ; Jahnke, T. S. Antiviral activities of isomeric dideoxynucleosides of D- and L-related stereochemistry. Antimicrob. Agents Chemother. 1995, 39, 1017-1029. (c) Marquez, V. E. Carbocyclic nucleosides. Adv. Antiviral Drug Design 1996, 2, 89-145. ; Gardiner, J. M. Acyclic nucleosides as antiviral compounds. Mol. Biotechnol. 1996, 5, 125-137. ; De Clercq, E. HPMPC (cidofovir), PMEA (adefovir) and related acyclic nucleoside phosphonate analogs: a review of their 54 G.
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