4-羟基喹啉-3-羧酸乙酯的合成及生物活性研究

Synthesis and biological activity of some ethyl 4-hydroxyquinoline-3-carboxylates

球虫病是家禽养殖业中最常见的寄生虫病之一,目前对该疾病最有效的防治手段是化学药物防治。伴随着现有药物纷纷由于耐药性而出现的疗效降低,开发新的抗球虫药物迫在眉睫。本文以邻苯基苯酚作为起始原料合成了一系列6-苄氧基-7-苯基-4-羟基喹啉-3-羧酸乙酯化合物,并利用1H NMR,13C NMR,和HR-MS等分析测试方法对化合物结构进行了表征,最后采用抗球虫指数(ACI)方法对目标化合物进行了生物活性测试,测试结果表明化合物5a和5f具有明显的抗球虫效果。

Coccidiosis is one of the most common parasitic diseases in poultry.The most effective means of prevention and treatment of this disease is chemical drug control.In this manuscript,a series of ethyl 6-benzyloxy-4-hydroxyquinoline-3-carboxylates with 7-phenyl groups were synthesized using o-phenylphenol as starting material,and the structure of the compounds were analyzed by1 H NMR,13 C NMR and HR-MS analytical methods.The biological activities were tested based on the Anticoccidial Index( ACI) method against Eimeria tenella in vivo,and the results showed that compounds 5 a,5 f displayed potent anticoccidial activities.