List of Contributors. Preface (E. De Clercq). From D- to L-nucleoside analogs as antiviral agents (J.G. Graciet, R.F. Schinazi). Orally bioavailable acyclic nucleoside phosphonate prodrugs: adefovir dipivoxil and BIS(POC)PMPA (M.N. Arimilli et al.). HEPT: from an investigation of lithiation of nucleosides towards a rational design of non-nucleoside reverse transcriptase inhibitors of HIV-1 (H. Tanaka et al.). Sialidase inhibitors as anti-influenza drugs (M. von Itzstein, J.C. Dyason). Bicyclam derivatives as HIV inhibitors (G.J. Bridger, R.T. Skerlj). Index.
Volume 3 of Advances in Antiviral Drug Design is keeping up with the recent progress made in the field of antiviral drug research and highlights five specific directions that have opened new avenues for the treatment of virus infections.
First, the use of lamivudine (3TC) for the treatment of HIV infections, and its more recent introduction for the treatment of hepatitis B virus (HBV) infections, has heralded the transition of D- to L-nucleosides in the antiviral nucleoside drug design, and it is likely that the future will provide more nucleosides of the L-configuration, such as (-)FFC (emtricitabine) and L-FMAU, as will be described by J.-C.G. Graciet and R.F. Shinazi.
Second, the acyclic purine nucleoside phosphonates, i.e. PMEA (adefovir and PMPA (tenofovir), offer great potential as both anti-HIV and anti-HBV agents, and both compounds have been the subject of advanced clinical trials in their oral produrg form (adefovir dipivoxil and tenofovir disoproxyl), as mentioned by M.N. Arimilli, J.P. Dougherty, K.C. Cundy, and N. Bischofberger.
Third, with the advent of nevirapine, delavirdine, and efavirenz, the NNRTIs have definitely come of age. Emivirine (MKC-442), a derivative of the original HEPT analog that was described in 1989 has now proceeded through pivotal clinical studies, and how this class of compounds evolved is presented in the account of H. Tanaka and his colleagues.
Fourth, at the end of 1999, anticipating on the next winter influenza offensive, we should have at end two compounds that specifically inhibit influenza A and B virus infections: zanamivir (by the intranasal route) and oseltamivir (by the oral route). Both compounds have proved effective in the prophylaxis and treatment of influenza A and B virus infections and act through the same mechanism; that is by blocking the viral neuraminidase (or sialidase), a key enzyme that allows the virus to spread f
For researchers and scientists interested in keepingup with the recent progress made in the field of antiviral drug research.
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- © Elsevier Science 1999
- 22nd November 1999
- Elsevier Science
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Rega Insitiute for Medical Research, Katholieke Universiteit Leuven, Belgium