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Lookup NU author(s): Suzanne Senior,
Dr Petr Illarionov,
Dr Sudagar Gurcha,
Professor David Minnikin,
Professor Del Besra
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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.
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
ISSN (print): 0960-894X
ISSN (electronic): 1464-3405
PubMed id: 14698162
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