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

By C.K. Chu

• up to date overview at the chemistry and biology of nucleosides • sleek artificial technique • complete assurance of antiviral nucleosidesThis ebook summarizes the new advances in nucleosides chemistry and chemotherapy over the last 10-15 years. It covers lately stumbled on nucleoside antiviral brokers, their healing points and biochemistry, and in addition wide stories on their chiral synthesis.

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Abstracts of Papers, 3rd International Conference on Therapies for Viral Hepatitis, Maui, USA; International Society for Antiviral Therapy: 1999; Abstract 119. Recent Advances in Antiviral Nucleosides 55 11. De Clercq, E. Vaccinia virus inhibitors as a paradigm for the chemotherapy of poxvirus infections. Clin. Microb. Rev. 2001,14, 382-397. 12. Chu, C. ; Pai, S. ; Sommadossi, J. ; Cheng, Y. -C. Use of 2'-fluoro-5-methyl-p-L-arabinofuranosyluracil as a novel antiviral agent for hepatitis B virus and Epstein-Barr virus.

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. Gumina, Y.

Chem. 1991,34,23832389. ; Herdewijn, P. Synthesis and antiviral activity of 5-thien-2-yl-2'-deoxyuridines. J. 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.

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