疟原虫组织期裂殖体杀灭剂的研究:2-取代苯氧基和4-甲基伯氨喹以及喹噁啉类衍生物的合成  

STUDIES ON THE TISSUE SCHIZONTICIDE OF MALARIA PARASITE:SYNTHESIS OF DERIVATIVES OF 2-SUBSTITUTED PHENOXYPRIMAQUINE,4-METHYLPRIMAQUINE AND QUINOXALINE

作　　者：陈昌[1] 郑贤育 郭惠珠 

机构地区：[1]中国预防医学科学院寄生虫病研究所,上海20002

出　　处：《药学学报》1992年第6期418-422,共5页Acta Pharmaceutica Sinica

摘　　要：合成了2-取代苯氧基伯氨喹及其类似物和4-甲基伯氨喹及其同系物以及7-甲氧基-5-(1-氨基烃基)氨基喹噁啉类化合物。其中以4-甲基伯氨喹的同分异构体25及其同系物24的作用最强。感染约氏疟原虫(Plasmodium yoelii)子孢子的小鼠,用10mg/kg单剂灌胃,全部小鼠的原虫血症均呈阴性,疗效高于对照组伯氨喹。2-Substituted phenoxy-, 4-methyl-6-methoxy-8-aminoquino-lines and 7-methoxy-5-aminoquinoxaline were condensed with 1-phthalimido-bromo-alkane to yield 2-substituted phenoxy-, 4-methyl-6-methoxy-8-(1-phthalimidoalkyl)-aminoquinolines(compounds7～10 and15～20) and 7-methoxy-5-(1-phthalimidoalkyl) aminoquinoxalines (28～30) which were subsequently reactedwith hydrazine hydrate to give 2-substituted phenoxy-,4-methyl-6-methoxy-8-(1-aminoalkyl)-aminoquinolines (11～14 and 22～27) and 7-methoxy-5-(1-aminoalkyl) aminoquinoxalines (31～33), respectively. The 2-substituted phenoxy-6-methoxy-8-aminoquinolines (4～6) were afforded by reduction of the corresponding 8-nitroquinolines (1～3) which were obtained by condensation of 2-chloro-6-methoxy-8-nitroquinoline and substituted phenols. Among them, compounds 25 and 24 were the most effective when evaluated inPlasmodium yoelli infected mice, no parasitemia was observed after a single oral dose of10 mg/kg.

关 键 词：4-甲基伯氨喹 疟原虫 杀虫剂 

分 类 号：R978.61[医药卫生—药品]