1-甲基-1,2,3,4-四氢异喹啉衍生物的合成及抗日本血吸虫活性评价

Synthesis and Evaluation of the Antischistosomal Activity against S.japonicum of 1-Methyl-1,2,3,4-tetrahydroisoquinoline Derivatives

大规模使用抗血吸虫病药物吡喹酮产生的耐药性问题备受关注．为了寻找新型的抗血吸虫病药物，设计、合成了一类1-甲基-1，2，3，4-四氢异喹啉衍生物2～10，并对化合物进行了体外抗日本血吸虫活性评价．结果显示，含有氯乙酰基取代的衍生物10表现了优于吡喹酮的杀虫活性，可以作为开发新型抗血吸虫病药物的先导化合物．

Due to widespread and intensive use of antischistosomal drug, praziquantel （PZQ）, there is serious concern that drug-resistant mutants of the parasite may emerge. To develop novel antischistosomal agents, a series of 1-methyl-1,2,3,4- tetrahydroisoquinoline derivatives were designed, synthesized, and evaluated for their antischistosomal activity against S. japonicum in vitro. The results indicated that compound 10 with chloroacetyl group showed better antischistosoaml activity than PZQ.