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Acetylene-based analogues of thiolactomycin, active against Mycobacterium tuberculosis mtFabH fatty acid condensing enzyme

Lookup NU author(s): Suzanne Senior, Dr Petr Illarionov, Dr Sudagar Gurcha, Professor David Minnikin, Professor Del Besra

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Abstract

Analogues of the natural antibiotic thiolactomycin, with acetylene-based side chains, have the highest recorded in vitro inhibitory activity against the recombinant Mycobacterium tuberculosis β-ketoacyl-ACP synthase mtFabH condensing enzyme. In particular, 5-[3-(4-acetyl-phenyl)-prop-2-ynyl]-4-hydroxy- 3,5-dimethyl-5H-thiophen-2-one exhibited more than an 18-fold increased potency, compared to thiolactomycin, against this key condensing enzyme, involved in M. tuberculosis mycolic acid biosynthesis. Analogues of the antibiotic thiolactomycin, with acetylene-based side chains, have the highest recorded activity against cloned mtFabH condensing enzyme. © 2003 Elsevier Ltd. All rights reserved.


Publication metadata

Author(s): Senior SJ, Illarionov PA, Gurcha SS, Campbell IB, Schaeffer ML, Minnikin DE, Besra GS

Publication type: Article

Publication status: Published

Journal: Bioorganic and Medicinal Chemistry Letters

Year: 2004

Volume: 14

Issue: 2

Pages: 373-376

ISSN (print): 0960-894X

ISSN (electronic): 1464-3405

Publisher: Pergamon

URL: http://dx.doi.org/10.1016/j.bmcl.2003.10.061

DOI: 10.1016/j.bmcl.2003.10.061

PubMed id: 14698162


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