| 光学活性益康唑和咪康唑的对映体选择性合成及其抗真菌活性 |
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| 引用本文： | 廖永卫,李鸿勋. 光学活性益康唑和咪康唑的对映体选择性合成及其抗真菌活性[J]. 药学学报, 1993, 0(1) |
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| 作者姓名： | 廖永卫 李鸿勋 |
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| 作者单位： | 第二军医大学化学教研室，第二军医大学化学教研室 上海 200433，上海 200433 |
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| 摘 要： | 首次用对映体选择性合成法制备了光学活性的益康唑和咪康唑。初步体外抗真菌活性试验结果表明,(R)-(—)-益康唑和(R)-(—)-咪康唑的抗真菌活性高于相应的(S)-异构体和外消旋体。
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| 关 键 词： | 光学活性 益康唑 咪康唑 对映体选择性合成 抗真菌活性 |
ENANTIOSELECTIVE SYNTHESIS AND ANTIFUNGAL ACTIVITY OF OPTICALLY ACTIVE ECONAZOLE AND MICONAZOLE |
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| YW Liao and HX Li. ENANTIOSELECTIVE SYNTHESIS AND ANTIFUNGAL ACTIVITY OF OPTICALLY ACTIVE ECONAZOLE AND MICONAZOLE[J]. Acta pharmaceutica Sinica, 1993, 0(1) |
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| Authors: | YW Liao and HX Li |
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| Abstract: | In an effort to investigate the relationship between stereochernistry and antifungal activity of the antimycotic agents, optically active econazole and miconazole were first enantioselectively synthesized. The key step was the enantioselective reduction of 2-chloro-1-(2,4-dichlorophenyl) ethanone catalyzed by chiral oxazaborolidine.Preliminary biological tests showed that (R)- (-)- econazole and ( R)- (-)- miconazole were more active than the (S)-isomer and racemates against common pathogenic fungi such as Candida albicans, Trichophyton rubrum, T. gypseum, Microsporum lanosum and Aspergillus flavus in vitro. |
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| Keywords: | Optically active Eeonazole Miconazole Enantioselective synthesis Antifungal activity |
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