| Design and synthesis of novel triazole antifungal derivatives based on the active site of fungal lanosterol 14a-demethylase （CYP51） |
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| 作者姓名： | Zhi Gang Dan Jun Zhang Shi Chong Yu Hong Gang Hu Xiao Yun Chai Qing Yan Sun Qiu Ye Wu |
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| 作者单位： | Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China |
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| 基金项目： | supported by the National Natural Science Foundation of China(No.20772153); by Shanghai Leading Academic Discipline Project(No.B906). |
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| 摘 要： | A series of 1-(1H-1,2,4-triazole-1-y1)-2-(2,4-difluorophenyl)-3-(N-isoproyl-N-substituted-amino)-2-propanols have been designed and synthesized on the basis of the active site of lanosterol 14a-demethylase(CYP51).Their structures were confirmed by MS and ~1H NMR.In vitro antifungal activities of these synthesized compounds were evaluated against eight human pathogenic fungi.The results showed that all title compounds exhibited activity against fungi tested to some extent.Compounds 3c,3d,7a,7b and 7c exhi...
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| 关 键 词： | 活性部位 抗真菌 醇合成 脱甲基酶 羊毛 设计 衍生物 三唑类 |
| 收稿时间： | 22 December 2008 |
Design and synthesis of novel triazole antifungal derivatives based on the active site of fungal lanosterol 14a-demethylase(CYP51) |
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| Zhi Gang Dan,Jun Zhang,Shi Chong Yu,Hong Gang Hu,Xiao Yun Chai,Qing Yan Sun,Qiu Ye Wu.Design and synthesis of novel triazole antifungal derivatives based on the active site of fungal lanosterol 14a-demethylase(CYP51)[J].Chinese Chemical Letters,2009,20(8):935-938. |
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| Authors: | Zhi Gang Dan Jun Zhang Shi Chong Yu Hong Gang Hu Xiao Yun Chai Qing Yan Sun Qiu Ye Wu |
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| Institution: | Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China |
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| Abstract: | A series of 1-(1H-1,2,4-triazole-1-y1)-2-(2,4-difluorophenyl)-3-(N-isoproyl-N-substituted-amino)-2-propanols have been designed and synthesized on the basis of the active site of lanosterol 14a-demethylase(CYP51).Their structures were confirmed by MS and ~1H NMR.In vitro antifungal activities of these synthesized compounds were evaluated against eight human pathogenic fungi.The results showed that all title compounds exhibited activity against fungi tested to some extent.Compounds 3c,3d,7a,7b and 7c exhibit... |
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| Keywords: | Triazole Synthesis Antifungal activity |
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