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

Sidath C. Kumarapperuma, Yanjie Sun, Marjan Jeselnik, Kiwon Chung, William B. Parker, Colleen B. Jonsson, Jeffrey B. Arterburn

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)3203-3207
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number11
DOIs
StatePublished - Jun 1 2007

Bibliographical note

Funding Information:
This work was supported by Department of Defense USAMRC Grant No. W81XWH-04-C-0055 (C.J.), and NIH INBRE RR016480 (J.A.).

Keywords

  • Adenosine kinase
  • Antiviral
  • Bioisostere
  • Ribavirin
  • Triazole

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