6-芳甲氧基-7-乙基-4-羟基-3-喹啉羧酸乙酯的合成及抗球虫活性研究

Synthesis and Anticoccidial Activities of Ethyl 6-arylmethoxy-7-ethyl-4-hydroxy-3-quinolinecarboxylates

鸡球虫病是由一种由艾美耳球虫引起的细胞内寄生虫病.目前,主要采用药物进行治疗.各类抗球虫药物在鸡球虫病的防治方面取得了巨大的成绩.其中,4-羟基-3-喹啉羧酸酯类化合物是一类重要的抗球虫药物.设计并合成了3个未见文献报道的6-芳甲氧基-7-乙基-4-羟基-3-喹啉羧酸乙酯类化合物.所有化合物的结构均经1H NMR,IR和HRMS等方法确证.对3个化合物进行了抗球虫活性实验,实验结果表明,在27 mg/kg的质量浓度下,化合物6-苄氧基-7-乙基-4-羟基-3-喹啉羧酸乙酯(5a)具有抗球虫活性.研究结果为进一步设计合成相关羟基喹啉羧酸酯类抗球虫化合物提供了一定的基础.

Coecidiosis is an intestinal infection caused by protozoan of the genus Eimeria. The disease has been controlled by the use of anticoceidial drugs. Various types of anticoccidial drugs have made great achievements in the prevention and treatment of coccid- iosis in chickens. Among them, 4-hydroxy-3-quinolinecarboxylates compounds are an important kind of anticoccidial drugs. Three ethyl 6-arylmethoxy-7-ethyl4-hydroxy-3-quinolinecarboxylates compounds are designed and synthesized in this paper. The structures of these compounds are confirmed by ~ H NMR, IR spectra and HRMS. Anticoccidial activities of these compounds are evaluated and the results indicate that ethyl 6-benzyloxy-7-ethyl4-hydroxy-3-quinolinecarboxylate （Sa） has anticoccidial activity against Eimeria in chicken＇ s diet with a dose of 27 mg/kg. The studies provide a certain foundation for expanding the research and applications of the derivatives of hydroxyl quinolinecarboxylate.