| 2-芳基苯并噁唑的合成和生物活性 |
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| 引用本文： | 冯志君,凌烈锋,金雅嫔.2-芳基苯并噁唑的合成和生物活性[J].皖南医学院学报,2012,31(3):180-182. |
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| 作者姓名： | 冯志君 凌烈锋 金雅嫔 |
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| 作者单位： | 1. 皖南医学院,化学教研室,安徽,芜湖,241002
2. 皖南医学院,生物化学教研室,安徽,芜湖,241002 |
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| 基金项目： | 安徽高校省级自然科学研究项目 |
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| 摘 要： | 目的:合成2-芳基苯并噁唑衍生物4a-d,测试化合物4b的生物活性。方法:用有机高价碘化合物醋酸碘苯(DIB)氧化苯酚亚胺分子内环化,生成目标化合物4a-d;采用打孔法测定4b对白念珠菌的抑制活性。结果:产物经过1H NMR,13C NMR,HRMS(EI)和IR等表征;生物活性测试表明,化合物4b在1μg/ml～1 mg/ml药剂浓度下对白念珠菌的抑菌圈直径为1.5～11.1 mm。结论:拓展了用有机高价碘试剂氧化环化形成2-芳基苯并噁唑衍生物的合成方法;化合物4b对白念珠菌有良好的抑制活性。
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| 关 键 词： | 苯并噁唑 醋酸碘苯(DIB) 合成 生物活性 |
Synthesis and biological activity of 2-arylbenzoxazole |
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| FENG Zhi-jun
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LING Lie-feng
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JIN Ya-pin.Synthesis and biological activity of 2-arylbenzoxazole[J].Acta Academiae Medicinae Wannan,2012,31(3):180-182. |
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| Authors: | FENG Zhi-jun LING Lie-feng JIN Ya-pin |
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| Institution: | Department of Chemistry,Wannan Medical University,Wuhu 241002,China |
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| Abstract: | Objective:To synthesize the 2-arylbenzoxazole and test the biological activities of these compounds.Methods:The title compounds 4a-d were synthesized via the oxidative intramolecular cyclization of the phenolic imines 3a-d,using iodobenzene diacetate(DIB) as an oxidant in methanol at room temperature.The antifungal activity against Candida albicans of 4b was tested.Results:The structures of the title compounds were characterized by IR,1H NMR,13C NMR and HRMS spectra.The diameters of inhibition zones against Candida albicans varied from 1.5 mm to 11.1 mm at the concentration of 4b from 1 μg/ml to 1 mg/ml.Conclusion:The results show that general method for the synthesis of 2-arylbenzoxazole using hypervalent iodine reagents and the compound 4b may facilitate antifungal activity against Candida albicans. |
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| Keywords: | benzoxazole iodobenzene diacetate(DIB) synthesis biological activity |
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