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Inhibition of escherichia coli glycosyltransferase MurG and mycobacterium tuberculosis Gal transferase by uridine-linked transition state mimics
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Trunkfield, Amy E., Gurcha, Sudagar S., Besra, Gurdyal S. and Bugg, Tim (2010) Inhibition of escherichia coli glycosyltransferase MurG and mycobacterium tuberculosis Gal transferase by uridine-linked transition state mimics. Bioorganic & Medicinal Chemistry, Vol.18 (No.7). pp. 2651-2663. doi:10.1016/j.bmc.2010.02.026 ISSN 0968-0896.
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Official URL: http://dx.doi.org/10.1016/j.bmc.2010.02.026
Abstract
Glycosyltransferase MurG catalyses the transfer of N-acetyl-D-glucosamine to lipid intermediate I on the bacterial peptidoglycan biosynthesis pathway, and is a target for development of new antibacterial agents. A transition state mimic was designed for MurG, containing a functionalised proline, linked through the alpha-carboxylic acid, via a spacer, to a uridine nucleoside. A set of 15 functionalised prolines were synthesised, using a convergent dipolar cycloaddition reaction, which were coupled via either a glycine, proline, sarcosine, or diester linkage to the 5'-position of uridine. The library of 18 final compounds were tested as inhibitors of Escherichia coli glycosyltransferase MurG. Ten compounds showed inhibition of MurG at 1 mM concentration, the most active with IC50 400 mu M. The library was also tested against Mycobacterium tuberculosis galactosyltransferase GlfT2, and one compound showed effective inhibition at 1 mM concentration. (C) 2010 Elsevier Ltd. All rights reserved.
Item Type: | Journal Article | ||||
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Subjects: | Q Science > QD Chemistry Q Science > QP Physiology Q Science > QR Microbiology |
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Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry | ||||
Library of Congress Subject Headings (LCSH): | Glycosyltransferases, Peptidoglycans -- Synthesis, Enzyme inhibitors, Mycobacterium tuberculosis, Escherichia coli | ||||
Journal or Publication Title: | Bioorganic & Medicinal Chemistry | ||||
Publisher: | Elsevier | ||||
ISSN: | 0968-0896 | ||||
Official Date: | April 2010 | ||||
Dates: |
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Volume: | Vol.18 | ||||
Number: | No.7 | ||||
Number of Pages: | 13 | ||||
Page Range: | pp. 2651-2663 | ||||
DOI: | 10.1016/j.bmc.2010.02.026 | ||||
Status: | Peer Reviewed | ||||
Publication Status: | Published | ||||
Access rights to Published version: | Restricted or Subscription Access | ||||
Funder: | Royal Society (Great Britain), Engineering and Physical Sciences Research Council (EPSRC), University of Warwick, Medical Research Council (Great Britain) (MRC), Wellcome Trust (London, England) | ||||
Grant number: | 081569/Z/06/Z (WT) |
Data sourced from Thomson Reuters' Web of Knowledge
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