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JAC Advance Access originally published online on September 1, 2003
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Journal of Antimicrobial Chemotherapy (2003) 52, 543-546
© 2003 The British Society for Antimicrobial Chemotherapy

Leading Article

Ribavirin, viramidine and adenosine-deaminase-catalysed drug activation: implication for nucleoside prodrug design

Jim Zhen Wu*, Chin-chung Lin and Zhi Hong

Drug Discovery and Development, Ribapharm Inc., 3300 Hyland Avenue, Costa Mesa, CA 92626, USA

Keywords: ribavirin, viramidine, hepatitis C virus, HCV, prodrugs

The first 150 words of the full text of this article appear below.

The epidemics caused by pathogenic viruses, such as HIV, hepatitis C virus (HCV) and most recently the severe acute respiratory syndrome (SARS) by a new coronavirus, represent major global health hazards, which demand novel broad-spectrum antiviral intervention. Although discovered 40 years ago, ribavirin (1-ß-D-ribofuranosyl-1,2,4-triazole-3-carboxamide) remains the only approved small molecule drug that is active against both DNA and RNA viruses.1 The unique antiviral profile of ribavirin deserves a brief review of its discovery. Back in the 1960s, two five-membered ring nucleoside antibiotics, showdomycin and pyrazomycin, were isolated from bacterial culture, and both (Figure 1) showed significant activity against a broad series of viruses in cell culture. The novel properties of these nucleoside antibiotics prompted synthesis and testing of a number of imidazole- and triazole-based ribonucleosides.2 Among them, ribavirin (originally termed Virazole) stood out as the most promising broad-spectrum antiviral agent. Structurally, ribavirin is a ribonucleoside with an . . . [Full Text of this Article]


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