Decoquinate (1 ) ,旧、便宜的 coccidiostat,展出有势力抗疟药活动然而,它对血吸虫 japonicum 的 antischistosomal 活动还没被评估了。基于 decoquinate,一系列 decoquinate 衍生物被设计,综合,与 S 作为 antischistosomal 代理人的一个新班作比较。在 vitro 的 japonicum 成年人蠕虫。在他们之中,混合 15 杀死的 100% 成年 S。在 72 的 japonicum ? 在 10 的集中的 h ? 在 vitro 的 mol/L,在 vitro 比 PZQ 展出了更强壮的杀死蠕虫的活动并且能用作有希望的铅混合物开发新 antischistosomal 代理人。
Decoquinate(1), an old and inexpensive coccidiostat, exhibited potent antimalarial activity, however, its antischistosomal activity against Schistosoma japonicum has not yet been evaluated. Based on decoquinate, a series of decoquinate derivatives was designed, synthesized, evaluated as a new class of antischistosomal agents against S. japonicum adult worms in vitro. Among them, compound 15 killed 100% of adult S. japonicum in 72 h at the concentration of 10 mmol/L in vitro, exhibited stronger wormkilling activity than PZQ in vitro and could serve as a promising lead compound to develop new antischistosomal agents.