摘要
合成了戊喹及其异构体 Win-5037以及它们的环取代衍生物14个。初步药理试验表明,大多数化合物对感染伯氏疟原虫的鼠的抑制性治疗显示中等活性,但除4-甲基衍生物(10a,b)外均低于伯氨喹。对鼠约氏疟原虫感染的病因性预防作用除4-甲基戊喹(10b),5-间氟苯氧基-2-苯氧基-Win-5037(9)外均不及伯氨喹。在猴疟根治试验中仅2-苯氧基-Win-5037(5a)的作用与伯氨喹相当。
The synthesis and antimalarial activity of pentaquine,its isomerWin-5037 and their fourteen ring-substituted derivatives are reported.Preliminaryscreening tests showed that most of the compounds appeared to have a moderateblood schizonticidal action but lower than that of primaquine except 4-methylpen-taquine(10b)and 4-methyl-Win-5037(10a).The causal prophylactic action onrodent malaria was much lower than primaquine except 10b and 2-phenoxy-5-(m-fluorophenoxy)-Win-5037(9).2-Phenoxy-Win-5037(5a)had the same radicalcurative acitivity against siminan malaria as primaquine.
出处
《医药工业》
CAS
1987年第5期210-215,共6页
