2-芳基苯并噁唑的合成和生物活性  被引量:1

Synthesis and biological activity of 2-arylbenzoxazole

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作  者:冯志君[1] 凌烈锋[2] 金雅嫔[1] 

机构地区:[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

出  处:《皖南医学院学报》2012年第3期180-182,共3页Journal of Wannan Medical College

基  金:安徽高校省级自然科学研究项目(KJ2009B109)

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。Objective :To synthesize the 2-arylbenzoxazole and test the bi- ological activities of these compounds. Methods : The title compounds 4a-d were synthesized via the oxidative intramolecular cyelization of the phenolic imines 3a-d,using iodobenzene diacetate(DIB) as an oxidant in meth- anol at room temperature. The antifungal activity against Candida albicans of 4b was tested. Results :The structures of the title compounds were char- acterized by IR, ~ H NMR, ~3 C NMR and HRMS spectra. The diameters of inhibition zones against Candida albieans 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 albieans.

关 键 词:苯并噁唑 醋酸碘苯(DIB) 合成 生物活性 

分 类 号:R914.4[医药卫生—药物化学]

 

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