CAJ | 학술논문

目的合成5-(3′-吲哚基)-噁唑衍生物并研究其抗氧化活性.方法以色氨酸为原料,与取代的苯甲酸在DCC催化下脱水缩合得到酰胺,再通过DDQ苄位氧化和分子内环合生成5-(3′-吲哚基)-噁唑.用DPPH体外抗氧化模型测定化合物的抗氧化活性.结果合成了11个2-取代苯基-5-(3′-吲哚基)-噁唑衍生物,其中化合物21和22的活性比维生素E强约3～4倍;化合物29的活性与维生素E相近.结论合成的目标化合物中有3个化合物有较好的抗氧化活性,有可能开发成为良好的抗氧化剂.
목적합성5-(3′-신타기)-오서연생물병연구기항양화활성.방법이색안산위원료,여취대적분갑산재DCC최화하탈수축합득도선알,재통과DDQ변위양화화분자내배합생성5-(3′-신타기)-오서.용DPPH체외항양화모형측정화합물적항양화활성.결과합성료11개2-취대분기-5-(3′-신타기)-오서연생물,기중화합물21화22적활성비유생소E강약3～4배;화합물29적활성여유생소E상근.결론합성적목표화합물중유3개화합물유교호적항양화활성,유가능개발성위량호적항양화제.
Aim To study the synthesis of 5-(3′-indolyl)-oxazoles and their antioxidative activity. Methods The amides were prepared from tryptophan and different acid derivatives by the catalytic dehydration of dicyclohexyl carbodiimide (DCC). The characteristic heterocyclic ring system of 5-(3′-indolyl)-oxazoles was constructed by oxidative cyclization of amide, using dicholorodicyanoquinone (DDQ). Their antioxidative activity in vitro was tested using DPPH system. Results Eleven 2-substituted phenyl-5-(3′-indolyl)-oxazoles were prepared, the compounds 21 and 22 have shown antioxidative activity 3-4 times stronger than that of Vit E, and the compound 29 showed antioxidative activity almost as same as Vit E. Conclusion Three 5-(3′-indoyl)-oxazole compounds synthesized showed potent antioxidative effect and they would be a good antioxidants.