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Phosphonate inhibitors of antigen 85C, a crucial enzyme involved in the biosynthesis of the Mycobacterium tuberculosis cell wall

  • S Gobec
  • , I Plantan
  • , J Mravljak
  • , Robert Wilson
  • , Gurdyal Besra
  • , D Kikelji

Research output: Contribution to journalLetter

29 Citations (Scopus)

Abstract

The first phosphonate inhibitors of antigen 85C-a major protein component of the Mycobacterium tuberculosis cell wall possessing mycolyltransferase activity were prepared using structure-based design. These potential novel antituberculosis agents, consisting of a phosphonate moiety, hydrophobic alkyl chain and a simple trehalose-mimicking aromatic structure, were designed as tetrahedral transition-state analogue inhibitors of antigen 85C, which catalyzes the key mycolyltransferase reaction involved in cell wall biosynthesis. (C) 2004 Elsevier Ltd. All rights reserved.
Original languageEnglish
Pages (from-to)3559-3562
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume14
Publication statusPublished - 1 Jan 2004

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

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