By C.K. Chu

• up to date evaluation at the chemistry and biology of nucleosides • sleek artificial method • entire insurance of antiviral nucleosidesThis ebook summarizes the hot advances in nucleosides chemistry and chemotherapy over the last 10-15 years. It covers lately came across nucleoside antiviral brokers, their healing features and biochemistry, and in addition broad reports on their chiral synthesis.

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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. Biochem. Pharmacol. 1983, 32, 3583-3590. 16. Harris, S. ; Balzarini, J. Synthesis and antiviral evaluation of phsphoramidate derivatives of (F)-5-(2-bromovinyl)-2'-deoxyuridine.

Med. Chem. 1993, 36, 538-543. 20. ; Lee, C. -C; Chu, C. K. Structure-activity relationships of (F)-5-(2-bromovinyl)uracil nucleosides and related analogs as anti-herpesvirus agents. /. Med. Chem. 2000, 43, 2538-2546. 21. Bryant, M. ; Bridges, E. ; Faraj. ; Loi, A. ; Imbach, J. ; Schinazi, R. ; Sonmiadossi, J. -P. Antiviral L-nucleosides specific for hepatitis B virus infection. Antimicrob.

5 |iM when dCTP is present at a concentration equal to its K^^ value. 3TCTP is a rather weak inhibitor of DNA polymerase y, but (±)-BCH-189 is about 650 times more inhibitory than 3TC, due to the activity of the D-isomer. ^^° Chain elongation studies with 3TC show that 3TCTP is incorporated into newly synthesized DNA and that transcription is terminated in similar fashion as seen with ddCTP. ^^^ Schinazi et al. have reported the anti-HIV activity of the racemates as well as the single enantiomers of the 5-fluoro congener of 3TC, FTC (emtricitabine, 114, 36 G.

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