By C.K. Chu

• updated evaluate at the chemistry and biology of nucleosides • smooth artificial technique • finished assurance of antiviral nucleosidesThis ebook summarizes the hot advances in nucleosides chemistry and chemotherapy during the last 10-15 years. It covers lately stumbled on nucleoside antiviral brokers, their healing facets and biochemistry, and likewise vast stories on their chiral synthesis.

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Fat" nucleosides. ^^ Structure-activity relationships of neplanocin A analogs revealed interesting antiviral activity. 2 and 15 |iM, respectively). ^^^ Recent Advances in Antiviral Nucleosides 53 NHp NH HO N-^N*^ OH HO ^ OH 183(neplanocinA) ^N'**0 ^ OH OH 184X = H 185X = F Figure 71. Neplanocin A and its D-cytidine analogs. ^^^ Its 5'-nor analog 187 is active against HCMV,^^^'^^'^ vaccinia virus and measles, while its (+)-enantiomer 188 is active against HBV. ^^^ X NHo 1 ^ N HO OH N - ^ N ^ Y OH OH 186 (aristeromycin) NH2 1 OH 1 8 7 X = NH2, Y = H 0::> N^^^N OH OH OH 188 1 8 9 X = OH, Y = NH2 Figure 72.

Enantioselectivity of the antiviral effects of nucleoside analogs. Pharmacol. Ther. 2000, 85, 251-266. ; Song, G. ; Chu, C. K. Advances in antiviral agents for hepatitis B virus. Antiviral Chem. Chemother. 2001, 72,89-112. 6. ; Young, R. J. Antiviral Chemotherapy Mann, J. ; Biochemical & Medicinal Chemistry Series; Spektrum: UK, 1997. (a) Crick, F. Life Itself, Simon and Shuster: New York, 1981. ; Focher, F. Lack of stereospecificity of some cellular and viral enzymes involved in the synthesis of deoxyribonucleotides and DNA: molecular basis for the antiviral activity of unnatural L-p-nucleosides.

Synthetic pyrimidine nucleoside analogs. In Approaches to Antiviral Agents, Hamden, M. ; Macmillan: London, 1985, pp. 57-99. (d) De Clercq, E. : London, 1988, Vol. 17, pp. 1-59. 14. ; Barr, P. ; Jones, A. ; Walker, R. T. (£r)-5-(2-Bromovinyl)2'-deoxyuridine: a potent and selective anti-herpes agent. Proc. Natl. Acad. Sci. USA 1979, 76, 29472951. 15. ; De Clercq, E. Phosphorolysis of (F)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) and other 5-substituted-2'-deoxyuridines by purified human thymidine phosphorylase and intact blood-platelets.

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Antiviral Nucleosides: Chiral Synthesis and Chemotherapy by C.K. Chu
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