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Biphenyl-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 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.


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: 2003

Volume: 13

Issue: 21

Pages: 3685-3688

ISSN (print): 0960-894X

ISSN (electronic): 1464-3405

Publisher: Pergamon

URL: http://dx.doi.org/v

DOI: 10.1016/j.bmcl.2003.08.015

PubMed id: 14552758


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