| 黄烷类衍生物的合成及其生物活性研究 |
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| 引用本文： | 何兰,孔婀静,刘玉美,安玉,张文生,史大华,谭仁详. 黄烷类衍生物的合成及其生物活性研究[J]. 中国化学, 2006, 24(3): 401-408. DOI: 10.1002/cjoc.200690077 |
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| 作者姓名： | 何兰 孔婀静 刘玉美 安玉 张文生 史大华 谭仁详 |
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| 作者单位： | [1]Department of Chemistry, Beijing Normal University, Beijing 100875, China [2]Protection and Utilization of Chinese Medicine Resources of Beijing Key Laboratory, Beifing Normal University, Beijing 100875, China [3]State Key Laboratory of Pharmaceutical Biotechnology, Institute of Functional Biomolecules, Nanjing University, Nanfing, Jiangsu 210093, China |
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| 基金项目： | Project supported by the Key Project of the Ministry of Education of China （No. 03013）, the National Natural Science Foundation of China （No. 20372010） and Trans-century Training Program Foundation for the Talents, Ministry of Education of China and Chinese Academy of Medical Sciences. |
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| 摘 要： | An efficient and feasible synthetic approach was developed for the synthesis of an array of new flavane derivafives from the substituted benzaldehyde with the reduction of chalcones and subsequent cyclization as the key steps. The purity and structure of the products were confirmed by the elemental analysis and a combination of its IR, ^1H and ^13C NMR, and mass spectra. These synthetic compounds were tested for xanthine oxidase （XO） inhibitions and antifungal actions against Candida albicans, Cryptococcus neoformans, Aspergillus sp. and Trichophyton rubrum. 7-Hydrazinocarbonylmethoxy-4＇-methoxyflavane （9） was found to be the most XO inhibitory with IC50=76.4 μmol/L, and the most potent antifungal compound was 4＇-hydrazinocarbonylmethoxyflavane （12） with minimal inhibition concentration MIC=8 μg/mL against Trichophyton rubrum.
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| 关 键 词： | 合成 生物活性 黄烷衍生物 黄嘌呤氧化酶 抗真菌作用 安息香醛 |
| 收稿时间： | 2005-08-04 |
| 修稿时间： | 2005-08-042005-12-28 |
Synthesis and Biological Activity of Flavane Derivatives |
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| He Lan;Kong EJing;Liu YuMei;An Yu;Zhang WenSheng;Shi DaHua;Tan RenXiang. Synthesis and Biological Activity of Flavane Derivatives[J]. Chinese Journal of Chemistry, 2006, 24(3): 401-408. DOI: 10.1002/cjoc.200690077 |
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| Authors: | He Lan Kong EJing Liu YuMei An Yu Zhang WenSheng Shi DaHua Tan RenXiang |
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| Abstract: | An efficient and feasible synthetic approach was developed for the synthesis of an array of new flavane derivatives from the substituted benzaldehyde with the reduction of chalcones and subsequent cyclization as the key steps. The purity and structure of the products were confirmed by the elemental analysis and a combination of its IR, 1H and 13C NMR, and mass spectra. These synthetic compounds were tested for xanthine oxidase (XO) inhibitions and antifungal actions against Candida albicans, Cryptococcus neoformans, Aspergillus sp. and Trichophyton rubrum. 7‐Hydrazinocarbonylmethoxy‐4′‐methoxyflavane ( 9 ) was found to be the most XO inhibitory with IC50=76.4 µmol/L, and the most potent antifungal compound was 4′‐hydrazinocarbonylmethoxyflavane ( 12 ) with minimal inhibition concentration MIC?8 μg/mL against Trichophyton rubrum. |
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| Keywords: | synthesis flavane derivative xanthine oxidase antifungal |
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