肝靶向抗疟药NGA－PQ的合成及其抗疟作用

HEPATIC TARGETING ANTIMALARIAL AGENT:SYNTHESIS AND ITS ANTIMALARIAL ACTIVITY

以肝细胞表面的无唾液酸糖蛋白受体的特异性配基──半乳糖基拟糖白蛋白（Ｎｅｏｇｌｙｃｏａｌｂｕｍｉｎ．ＮＧＡ）作为载体，通过丁二酰胺桥，成功地与抗疟药伯氨喹（ＰＱ）偶联，制备了肝靶向抗疟药ＮＧＡ－ＰＱ，药密度达到１６．８±０．８５，糖密度达到２１．７±１．７３．经药效学试验，ＮＧＡ－ＰＱ的抗疟作用明显优于同剂量的ＰＱ。

Neoglycoalbumin(NGA),the special ligend of asialoglycoprotein receptor on the hepatocyte,was linked via a butanediamide bridge to the free amino group of primaquine to form a conjugator NGA-PQ,The drug density and carbohydrate density of the NGA-PQ which was used as a hepatic antimalarial agent were 16.8±0.85 and 21.7±1. 73 respectively. The study on its therapeutic activity demonstrated that the antimalaria activity of half dose of PQ in NGA-PQ was more effective than that of the same dose of PQ.