Design and synthesis of chitin synthase inhibitors as potent fungicides

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 bacte...

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Bibliographic Details
Published in:Chinese chemical letters 2017-06, Vol.28 (6), p.1232-1237
Main Authors: Chen, Qi, Zhang, Ji-Wei, Chen, Lu-Lu, Yang, Jun, Yang, Xin-Ling, Ling, Yun, Yang, Qing
Format: Article
Language:English
Subjects:
Chitin synthase
Fungicide
Inhibitor
UDP-N-acetyl-D-glucosamine
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Summary: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 IC（50） 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.
ISSN:1001-8417
1878-5964
DOI:10.1016/j.cclet.2017.03.030