New hepatitis C virus research from F. Hoffmann-LaRoche Ltd. described
2009 JUL 13 - (NewsRx.com) -- According to a study from the United States, "The discovery of 4'-azidocytidine (3) (R1479) (J. Biol. Chem. 2006, 281, 3793; Bioorg. Med. Chem. Lett. 2007, 17, 2570) as a potent inhibitor of RNA synthesis by NS5B (EC50 = 1.28 mc M), the RNA polymerase encoded by hepatitis C virus (HCV), has led to the synthesis and biological evaluation of several monofluoro and difluoro derivatives of 4'-azidocytidine." "The most potent compounds in this series were 4'-azido-2'-deoxy-2',2'-difluorocytidine and 4'-azido-2'-deoxy-2'-fluoroarabinocytidine with antiviral EC50 of 66 nM and 24 nM in the HCV replicon system, respectively," wrote D.B. Smith and colleagues, F. Hoffmann-LaRoche Ltd.. The researchers concluded: "The structure-activity relationships within this series were discussed. which led to the discovery of these novel nucleoside analogues with the most potent compound, showing more than a 50-fold increase in antiviral potency as compared to 4'-azidocytidine (3)." Smith and colleagues published their study in the Journal of Medicinal Chemistry (The Design, Synthesis, and Antiviral Activity of Monofluoro and Difluoro Analogues of 4'-Azidocytidine against Hepatitis C Virus Replication: The Discovery of 4'-Azido-2'-deoxy-2'-fluorocytidine and 4'-Azido-2'-dideoxy-2',2'-difluorocytidine. Journal of Medicinal Chemistry, 2009;52(9):2971-2978). For more information, contact M. Smith, Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. Publisher contact information for the Journal of Medicinal Chemistry is: American Chemical Society, 1155 16th St., NW, Washington, DC 20036, USA. Keywords: United States, Palo Alto, Antiviral Activity, Enzyme Research, Gastroenterology, HCV, Hepatitis C Virus, Hepatology, Infectious Disease, Medicinal Chemistry, Polymerase, Therapy, Treatment, Viral Inhibition, Viral Therapy, Virology, F. Hoffmann-LaRoche Ltd.. This article was prepared by Hepatitis Weekly editors from staff and other reports. Copyright 2009, Hepatitis Weekly via NewsRx.com.
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