Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies

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• 作者：Dongmei Zhao^a ; ^{medchemzhao@163.com} ; Shizhen Zhao^a ; Liyu Zhao^a ; Xiangqian Zhang^a ; Peng Wei^a ; Chunchi Liu^a ; Chenzhou Hao^a ; Bin Sun^c ; Xin Su^b ; ^{suxin1966@163.com} ; Maosheng Cheng^a
• 关键词：Antifungal activity ; CYP51 ; Structure-activity relationship ; Azole antifungals
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：25
• 期：2
• 页码：750-758
• 全文大小：1035 K
• 卷排序：25

文摘

27 new compounds with biphenyl imidazole scaffolds were designed and synthesized. Compounds 12f–g and 19a–b showed better antifungal activity than fluconazole. The structure-activity relationships of compounds were discussed. Mechanism studies revealed that the 12g might act by inhibiting the CYP51.