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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 antibiotic thiolactomycin, with biphenyl-based 5-substituents, were found to have excellent in vitro inhibitory activity against the recombinant Mycobacterium tuberculosis β-ketoacyl-ACP synthase mtFabH condensing enzyme. In particular, 5-(4′ -benzyloxy-biphen-4-ylmethyl)-4-hydroxy-3,5-dimethyl-5H-thiophen-2-one exhibited approximately a 4-fold increased potency against this key condensing enzyme involved in M. tuberculosis mycolic acid biosynthesis, compared to thiolactomycin. © 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: 14552758
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