Synthesis and antifungal activities in vitro of novel pyrazino [2,1-a] isoquinolin derivatives

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• 作者：Hui Tang ; Canhui Zheng ; Jiaguo Lv ; Juan Wu ; Yanan Li ; Hui Yang ; Bingyue Fu ; Chuntong Li ; Youjun Zhou ; Ju Zhu
• 关键词：Antifungal ; Pyrazino[2 ; 1-a]isoquinoline ; Lanosterol 14α ; -demethylase(CYP51) ; Synthesis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 February 2010
• 年：2010
• 卷：20
• 期：3
• 页码：979-982
• 全文大小：400 K

文摘

A series of novel pyrazino[2,1-a]isoquinolin compounds were designed and synthesized, and their antifungal activities in vitro were evaluated. The results showed that all of the compounds exhibited antifungal activities. Some of them exhibited stronger antifungal activities than that of lead compounds and among them compound 11b was the most potent one, which showed more potent than that of the active control fluconazole to the four of the five tested fungi. The studies presented here provide a new structural type for the development of novel antifungal agents.