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.
出处
《皖南医学院学报》
CAS
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)
关键词
苯并噁唑
醋酸碘苯(DIB)
合成
生物活性
benzoxazole
iodobenzene diacetate （ DIB ）
synthesis
bio- logical activity
