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Design and Synthesis of Novel Pyrazino[2,1‐a]isoquinolin Derivatives with Potent Antifungal Activity
Authors:Hui Tang  Can‐hui Zheng  Ju Zhu  Bing‐yue Fu  You‐jun Zhou  Jia‐guo Lv
Affiliation:1. School of Pharmacy, Second Military Medical University, Shanghai, P. 2. R. China. Fax: +86 21 818‐7123‐1
Abstract:A series of novel pyrazino[2,1‐a]isoquinolin compounds were designed, synthesized, and their antifungal activities in vitro were evaluated. The results showed that all of the title compounds exhibited antifungal activities. Most of them exhibited stronger antifungal activities than the lead compounds; compound 7c is more potent than fluconazole against two of the three tested fungal strains. The studies presented here provide a new structural type for the development of novel antifungal agents.
Keywords:Antifungal  Lanosterol 14α  ‐demethylase  Pyrazino[2,1‐a]isoquinolin  Synthesis
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