湖南师范大学自然科学学报
湖南師範大學自然科學學報
호남사범대학자연과학학보
ACTA SCIENTIARUM NATURALIUM UNIVERSITATIS NORMALIS HUNANENSIS
2013年
4期
49-52
,共4页
二茂铁基%喹喔啉%抗疟活性%恶性疟原虫
二茂鐵基%喹喔啉%抗瘧活性%噁性瘧原蟲
이무철기%규악람%항학활성%악성학원충
ferrocenyl%quinoxaline%antimalarial activity%plasmodium falciparum
以二茂铁甲醛为起始原料,经过6步反应合成得到新型的二茂铁吡咯并[1,2-α]喹喔啉哌嗪类衍生物1a-h.产物针对恶性疟原虫FcB1, K1, F32等菌株进行了体外抑制活性实验.实验结果表明,新合成的化合物具有一定的抗疟活性,其中芳环上4-位硝基取代的化合物1h体外抗疟活性最优.本工作为进一步研究具有更好活性的抗疟药物打下一定的基础.
以二茂鐵甲醛為起始原料,經過6步反應閤成得到新型的二茂鐵吡咯併[1,2-α]喹喔啉哌嗪類衍生物1a-h.產物針對噁性瘧原蟲FcB1, K1, F32等菌株進行瞭體外抑製活性實驗.實驗結果錶明,新閤成的化閤物具有一定的抗瘧活性,其中芳環上4-位硝基取代的化閤物1h體外抗瘧活性最優.本工作為進一步研究具有更好活性的抗瘧藥物打下一定的基礎.
이이무철갑철위기시원료,경과6보반응합성득도신형적이무철필각병[1,2-α]규악람고진류연생물1a-h.산물침대악성학원충FcB1, K1, F32등균주진행료체외억제활성실험.실험결과표명,신합성적화합물구유일정적항학활성,기중방배상4-위초기취대적화합물1h체외항학활성최우.본공작위진일보연구구유경호활성적항학약물타하일정적기출.
A series of novel ferrocenyl-substituted pyrrolo [1,2-α] quinoxaline piperazines 1a-h were synthe-sized from ferrocene-carboxaldehyde by six-step reactions .All of the compounds were screened for their antimalarial activities against plasmodium falciparum FcB1, K1, F32 strains.The results revealed that compounds 1 exhibited some inhibitory activities against the plasmodium falciparum strains.Among them, nitro substituted 1h was best. This work laid a foundation for further study of new antimalarial drugs .