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Issue 36, 2016
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Efficient total syntheses and biological activities of two teixobactin analogues

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Abstract

The discovery of the new antibiotic teixobactin has been timely in the race for unearthing novel antibiotics wherein the emergence of drug resistant bacteria poses a serious threat worldwide. Herein, we present the total syntheses and biological activities of two teixobactin analogues. This approach is simple, efficient and has several advantages: it uses commercially available building blocks (except AllocHN-D-Thr-OH), has a single purification step and a good recovery (22%). By using this approach we have synthesised two teixobactin analogues and established that the D-amino acids are critical for the antimicrobial activity of these analogues. With continuing high expectations from teixobactin, this work can be regarded as a stepping stone towards an in depth study of teixobactin, its analogues and the quest for synthesising similar molecules.

Graphical abstract: Efficient total syntheses and biological activities of two teixobactin analogues

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Publication details

The article was received on 13 Dec 2015, accepted on 09 Mar 2016 and first published on 09 Mar 2016


Article type: Communication
DOI: 10.1039/C5CC10249A
Citation: Chem. Commun., 2016,52, 6060-6063
  • Open access: Creative Commons BY license
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    Efficient total syntheses and biological activities of two teixobactin analogues

    A. Parmar, A. Iyer, C. S. Vincent, D. Van Lysebetten, S. H. Prior, A. Madder, E. J. Taylor and I. Singh, Chem. Commun., 2016, 52, 6060
    DOI: 10.1039/C5CC10249A

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