Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents
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- 作者：Qinggang Jia ; jiqing@swu.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Zhiqiang Gea ; Zhixing Gec ; Kaizhi Chena ; Hualong Wua ; Xiaofei Liua ; Yanrong Huanga ; Lvjiang Yuana ; Xiaolan Yangb ; Fei Liaob
- 关键词：Coumarin ; Phosphoramidate ; Chitin synthase inhibitor ; Antifungal agents
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：27 January 2016
- 年：2016
- 卷：108
- 期：Complete
- 页码：166-176
- 全文大小：674 K
文摘
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A serial of novel phosphoramidate derivatives of coumarin were designed.
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These compounds exhibited moderate to excellent activity against chitin synthase.
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These compounds showed good activity against the main pathogenic fungi in clinic.
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The 7t was a non-competitive inhibitor with apparent Ki values of 0.096 mM.