| 1-(1H-1,2,4-三唑-1-基)-(2,4-二氟苯基)-3-(N-环己基-N-取代氨基)-2-丙醇的合成及抗真菌活性 |
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| 引用本文： | 吴玮峰,杨志辉,但志刚,薛云云,胡宏岗,柴晓云,俞世冲,吴秋业. 1-(1H-1,2,4-三唑-1-基)-(2,4-二氟苯基)-3-(N-环己基-N-取代氨基)-2-丙醇的合成及抗真菌活性[J]. 药学实践杂志, 2009, 27(4): 266-269 |
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| 作者姓名： | 吴玮峰 杨志辉 但志刚 薛云云 胡宏岗 柴晓云 俞世冲 吴秋业 |
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| 作者单位： | 1. 第二军医大学药学院有机化学教研室,上海,200433
2. 空军总医院药学部,北京,100142 |
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| 基金项目： | 国家自然科学基金资助项目，上海市重点学科资助项目 |
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| 摘 要： | 目的：以氟康唑为先导化合物，设计合成新的三唑醇类化合物，并研究其抗真菌活性。方法：引入环己基侧链结构，合成一系列目标化合物，所有化合物结构均经Ms、1H—NMR等谱确证；选择8种真菌为实验菌株，测定其体外抗真菌活性。结果：合成了11个未见文献报道的目标化合物，部分化合物对所选真菌均表现出了一定的抑菌活性。结论：引入环己基对抗真菌活性影响较大。
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| 关 键 词： | 三唑醇衍生物 合成 环己基 抗真菌活性 |
| 收稿时间： | 2009-04-29 |
Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols |
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| WU Wei-feng,YANG Zhi-hui,DAN Zhi-gang,XUE Yun-yun,HU Hong-gang,CHAI Xiao-yun,YU Shi-chong and WU Qiu-ye. Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-benzyl-amino)-2-propanols[J]. The Journal of Pharmaceutical Practice, 2009, 27(4): 266-269 |
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| Authors: | WU Wei-feng YANG Zhi-hui DAN Zhi-gang XUE Yun-yun HU Hong-gang CHAI Xiao-yun YU Shi-chong WU Qiu-ye |
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| Affiliation: | Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Pharmcy, Air force general hospital, Beijing 100142, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China |
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| Abstract: | Objective:Design and synthesis of novel triazole antifungal derivatives based on the structure of fluconazole.Methods: A cyclohexyl group introduced and a series title compounds synthesized All of them were confirmed by MS,1H-NMR,et al.The antifungal activities were also evaluated against the eight common pathogenic fungi.Results:Eleven title compounds were synthesized.Some of the title compounds exhibited activity against fungi tested to some extent.Conclusion:A cyclohexyl group introduced to the side chain affected the antifungal activity. |
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| Keywords: | triazole synthesis cyclohexyl antifungal activity |
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