1981年,A.Trouet等报道了伯喹的氨基酸(亮氨酸)和肽类(丙氨酰——亮氨酸;丙氨酰——亮氨酰——丙氨酰——亮氨酸)衍生物作为前体药物,可降低伯喹的毒性并提高疗效。从报道的初步药理结果来看,二肽和四肽衍生物有降低毒性和提高疗效的作用。为寻找新的长效、低毒的伯喹衍生物,我们在过去研究工作的基础上又设计合成了一些不同于国外文献已报道的新衍生物: In 1981, A.Trouet et al. Reported on the amino acids (leucine) and peptides (alanyl-leucine; alanyl-leucyl-alanyl-leucine) Derivatives as prodrugs reduce primaquine toxicity and improve efficacy. From the preliminary pharmacological results reported, dipeptide and tetrapeptide derivatives have the effect of reducing toxicity and improving curative effect. In order to find a new long-acting and low-toxicity primary quinoline derivative, we have designed and synthesized some new derivatives which have been reported in foreign literature based on the previous research work: