Citation: Chen Qi, Zhang Ji-Wei, Chen Lu-Lu, Yang Jun, Yang Xin-Ling, Ling Yun, Yang Qing. Design and synthesis of chitin synthase inhibitors as potent fungicides[J]. Chinese Chemical Letters, ;2017, 28(6): 1232-1237. doi: 10.1016/j.cclet.2017.03.030 shu

Design and synthesis of chitin synthase inhibitors as potent fungicides

  • Corresponding author: Ling Yun, lyun@cau.edu.cn Yang Qing, qingyang@dlut.edu.cn
  • 1These authors contributed equally to this work
  • Received Date: 17 February 2017
    Revised Date: 19 March 2017
    Accepted Date: 21 March 2017
    Available Online: 24 June 2017

Figures(3)

  • Chitin is a structural component of fungal cell walls but is absent in vertebrates, mammals, and humans. Chitin synthase is thus an attractive molecular target for developing fungicides. Based on the structure of its donor substrate, UDP-N-acetyl-glucosamine, as well as the modelled structure of the bacterial chitin synthase NodC, we designed a novel scaffold which was then further optimized into a series of chitin synthase inhibitors. The most potent inhibitor, compound 13, exhibited high chitin synthase inhibitory activity with an IC50 value of 64.5 μmol/L. All of the inhibitors exhibited antifungal activities against the growth of agriculturally-destructive fungi, Fusarium graminearum, Botrytis cinerea, and Colletotrichum lagenarium. This work presents a new scaffold which can be used for the development of novel fungicides.
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    27. [27]

      Zhang J., Li Y., Yang X.. Synthesis and bioactivities of nucleoside compounds containing substituted benzoyl carbamate thiourea[J]. Chin. J. Org. Chem., 2013,33:305-311. doi: 10.6023/cjoc201210036

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      Ke S., Liu F., Wang N.. 1, 3, 4-Oxadiazoline derivatives as novel potential inhibitors targeting chitin biosynthesis:design, synthesis and biological evaluation[J]. Bioorg. Med. Chem. Lett., 2009,19:332-335. doi: 10.1016/j.bmcl.2008.11.095

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