Besra, Gurdyal

Gobec, S

Kikelji, D

Mravljak, J

Plantan, I

Wilson, Robert

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

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

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