Structural effects on the phosphorylation of 3-substituted 1-β-D-ribofuranosyl-1, 2, 4-triazoles by human adenosine kinase

…, K Chung, WB Parker, CB Jonsson, JB Arterburn

Index: Kumarapperuma, Sidath C.; Sun, Yanjie; Jeselnik, Marjan; Chung, Kiwon; Parker, William B.; Jonsson, Colleen B.; Arterburn, Jeffrey B. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 11 p. 3203 - 3207

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Citation Number: 14

Abstract

The conversion of ribavirin to the monophosphate by adenosine kinase is the rate-limiting step in activation of this broad spectrum antiviral drug. Variation of the 3-substituents in a series of bioisosteric and homologated 1-β-d-ribofuranosyl-1, 2, 4-triazoles has marked effects on activity with the human adenosine kinase, and analysis of computational descriptors and binding models offers insight for the design of novel substrates.