Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents
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- 作者：Shizhen Zhaoa ; Liyu Zhaoa ; Xiangqian Zhanga ; Chunchi Liua ; Chenzhou Haoa ; Honglei Xiea ; Bin Sunb ; Dongmei Zhaoa ; medchemzhao@163.com" class="auth_mail" title="E-mail the corresponding author ; Maosheng Chenga
- 关键词：Antifungal activity ; Azole antifungals ; CYP51 ; Structure-activity relationship
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 November 2016
- 年：2016
- 卷：123
- 期：Complete
- 页码：514-522
- 全文大小：706 K
文摘
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25 new compounds with benzothiazole scaffolds were designed and synthesized.
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Compounds 14j, 14o-r and 19a-b showed better antifungal activity than fluconazole.
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14p displayed moderate activity against Fluconazole-resistant of Candida albicans.
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The structure-activity relationships of compounds were discussed.
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Mechanism studies revealed that the 14p might act by inhibiting the CYP51.