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

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 journal › Letter

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 language	English
Pages (from-to)	3559-3562
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	14
Publication status	Published - 1 Jan 2004

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

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.",

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year = "2004",

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T1 - Phosphonate inhibitors of antigen 85C, a crucial enzyme involved in the biosynthesis of the Mycobacterium tuberculosis cell wall

AU - Gobec, S

AU - Plantan, I

AU - Mravljak, J

AU - Wilson, Robert

AU - Besra, Gurdyal

AU - Kikelji, D

PY - 2004/1/1

Y1 - 2004/1/1

N2 - 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.

AB - 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.

M3 - Letter

C2 - 15177473

VL - 14

SP - 3559

EP - 3562

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

ER -

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

Abstract

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