N-取代四氢异喹啉衍生物的合成及杀多子小瓜虫研究  

Synthesis and Antiparasitic Activity against Protozoan Parasite Ichthyophthirius multifiliis of N-Substituted-Tetrahydroisoquinoline Derivatives

作　　者：姚嘉赟[1] 张成赛 尹文林[1] 蔺凌云[1] 潘晓艺[1] 曹铮[1] 刘忆翰 夏炎春 沈锦玉[1] YAO Jiayun;ZHANG Chengsai;YIN Wenlin;LIN Lingyun;PAN Xiaoyi;CAO Zheng;LIU Yihan;XIA Yanchun;SHEN Jinyu(Key Laboratory of Healthy Freshwater Aquaculture,Ministry of Agriculture and Rural Affairs,Key Laboratory of Fish Health and Nutrition of Zhejiang Province,Zhejiang Institute of Freshwater Fisheries,Huzhou 313001,China;College of Animal Science and Technology,Jilin Provincial Engineering Research Center of Animal Probiotics,Key Laboratory of Animal Production and Product Quality Safety,Ministry of Education,Jilin Agricultural University,Changchun 130118,China)

机构地区：[1]浙江省淡水水产研究所,浙江省鱼类健康与营养重点实验室,农业农村部淡水渔业健康养殖重点实验室,浙江湖州313001 [2]吉林农业大学动物科技学院,吉林省动物微生态制剂工程研究中心,吉林长春130118

出　　处：《水产科学》2021年第5期768-773,共6页Fisheries Science

基　　金：浙江省公益技术应用研究项目(LGN18C190005,2014C32055);浙江省科技计划项目(2017F30034,2018C02033).

摘　　要：以苯乙醇为起始原料,对醇基的α位碳上的氢进行取代,反应合成3种N-取代四氢异喹啉衍生物(化合物1~3),研究其对多子小瓜虫掠食体和包囊的杀虫活性,评价杀虫活性物质的安全性。试验结果表明,合成的3种四氢异喹啉衍生物对多子小瓜虫的掠食体和包囊均具有一定的杀灭作用,其中化合物1(2-甲胺基-1,2,3,4-四氢异喹啉-1-甲腈)的杀虫活性最强,其对多子小瓜虫掠食体4h的100%灭杀质量浓度为20.0mg/L,对包囊6h的100%灭杀质量浓度为40.0mg/L,对掠食体的半数致死质量浓度为11.6mg/L。急性毒性试验结果显示,化合物1对翘嘴红鲌的48h半致死质量浓度为62.78mg/L。2-甲胺基-1,2,3,4-四氢异喹啉-1-甲腈具有较好的体外杀多子小瓜虫活性,且毒性较低,具有较好的开发潜力。Three N-substituted-tetrahydroisoquinoline derivatives were designed,synthesized,and evaluated for their antiparasitic activity against protozoan parasite Ichthyophthirius multifiliis in vitro.The toxicity of the synthesized N-substituted-tetrahydroisoquinoline derivatives was also evaluated to develop novel antiparasitic agents against the protozoan parasite.The results showed that there was promising antiparasitic activity against I.multifiliis theronts and encysted tomonts in vitro in all the three synthesized compounds,with the maximal activity against I.multifiliis in compound 1(2-methylamino-1,2,3,4-tetrahydroisoquinoline-formonitrile).The compound 1 had 100%effective against theronts at concentration of 20.0 mg/L in 4 h,with the median lethal concentration(LC_(50))of 11.6 mg/L.All dead encysted tomonts were observed in compound 1 at concentration of 40.0 mg/L,with the compound 148 h LC_(50) of 62.78 mg/L for topmouth culter Erythroculter ilishaeformis.The findings indicated that compound 1(2-methylamino-1,2,3,4-tetrahydroisoquinoline-formonitrile)was useful in aquaculture for control of I.multifiliis due to high antiparasitic efficacy against I.multifiliis with low toxicity.

关 键 词：异喹啉衍生物 掠食体 包囊 多子小瓜虫 

分 类 号：S941.5[农业科学—水产养殖]