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- Volume 4, Issue 2, 2005
Current Medicinal Chemistry - Anti-Infective Agents - Volume 4, Issue 2, 2005

Volume 4, Issue 2, 2005
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Editorial [Hot Topic:Human Immunodeficiency Virus (HIV) and Hepatitis C Virus (HCV) (Guest Editor: Christopher J. Burns)]
More LessThis Issue of Current Medicinal Chemistry - Anti-Infective Agents focuses principally on two of the major viral pathogens impacting human health, morbidity and mortality - Human Immunodeficiency Virus (HIV) and Hepatitis C Virus (HCV). The selected reviews center on recent progress made on therapeutic targets that are creating optimism within the pharmaceutical and medical communities. Currently marketed HIV therapie Read More
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Allosteric Inhibitors of Hepatitis C NS5B RNA-dependent RNA Polymerase°
Authors: Stephen M. Condon, Matthew G. LaPorte and Torsten HerbertzInfection with HCV is a global concern. Estimates from the WHO suggest that over 170 million people are infected worldwide with over 2.7 million people infected in the US. Current therapies including interferon (IFN-α) and ribavirin are ineffective against many HCV genotypes and a sustained viral response is difficult to achieve in many HCV patients. Inconvenient dosing regimens and overall toxicity conspire to make these curr Read More
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Dynamics and Structure-based Design of Drugs Targeting the Critical Serine Protease of the Hepatitis C Virus - From a Peptidic Substrate to BILN 2061
Authors: Steven R. LaPlante and Montse Llinàs-BrunetHepatitis C virus (HCV) infection is a serious cause of chronic liver disease worldwide. Although a treatment of limited efficacy exists, there is an urgent need for potent antivirals that can specifically target the viral proteins that are essential for replication. We recently reported the discovery of BILN 2061, a selective and potent inhibitor of the HCV NS3 protease. When administered to HCV infected patients for two days, BILN Read More
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Recent Progress in the Discovery of New CCR5 and CXCR4 Chemokine Receptor Antagonists as Inhibitors of HIV-1 Entry. Part 2*
This review addresses key medicinal chemistry issues relevant in the discovery and development of CCR5 and CXCR4 antagonists as anti-HIV drugs. Recent progress in the discovery and development of such antagonists, SAR and clinical status are reviewed.
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Identification of Authentic Inhibitors of HIV-1 Integration
Authors: M. Witvrouw, V. Fikkert, J. Vercammen, B. V. Maele, Y. Engelborghs and Z. DebyserCurrent strategies for the treatment of human immunodeficiency virus (HIV) infection are based on cocktails of drugs that target the viral entry step and the enzymes reverse transcriptase or protease. At present, the clinical benefit of this combination therapy for HIV-infected patients is considerable, although it is not clear how long this effect will last taking into account the emergence of multiple drug-resistant viral strai Read More
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Arylsulphones: A Promising Class of Non-Nucleoside Antiviral Agents
Authors: Laura Garuti, Marinella Roberti, Daniela Pizzirani and Gabriella PoggiThe design and development of antiviral agents are an urgent need. The continuing problem associated with the emergence of drug resistant strains stimulates for new compounds for the treatment of both chronic diseases and acute infections. A large number of arylsulphones have been reported to show potent antiviral activity. Although they have a common chemical feature, an aromatic heterocycle bearing a sulphonyl Read More
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