Analogues of SB-203207 as inhibitors of tRNA synthetases

Martin G. Banwell, Curtis F. Crasto, Christopher J. Easton*, Andrew K. Forrest, Tomislav Karoli, Darren R. March, Lucy Mensah, Michael R. Nairn, Peter J. O'Hanlon, Mark D. Oldham, Weimin Yue

*Corresponding author for this work

    Research output: Contribution to journalArticlepeer-review

    79 Citations (SciVal)

    Abstract

    SB-203207 and 10 analogues have been prepared, by elaboration of altemicidin, and evaluated as inhibitors of isoleucyl, leucyl and valyl tRNA synthetases (IRS, LRS, and VRS, respectively). Substituting the isoleucine residue of SB-203207 with leucine and valine increased the potency of inhibition of LRS and VRS, respectively. The leucine derivative showed low level antibacterial activity, while several of the compounds inhibited IRS from Staphylococcus aureus WCUH29 more strongly than rat liver IRS. (C) 2000 Elsevier Science Ltd.

    Original languageEnglish
    Pages (from-to)2263-2266
    Number of pages4
    JournalBioorganic and Medicinal Chemistry Letters
    Volume10
    Issue number20
    DOIs
    Publication statusPublished - 16 Oct 2000

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