Anti-protazoal 1,2,4-oxsdiuok derivatives of the formula:
wherein R1 is amino or substituted amino; each R2 is the same or different in one or more of the 3, 4, 5 or 6 positions and is hydrogen, lower alkyl, halogen. hydroxy, alkoxy, alkytthio, arytthio, amino, substituted amino, cyano or nitro: X and Y together represent a bond or X and Y are both hydrogen; R3 is hydrogen, lower alkyl, aryl, substituted aryl or ArS.CH2-; and Ar is unsubstituted or mono-, di- or tri-substituted phenyl wherein the substituents may be the same or different, and acid addition salts thereof, methods for their preparation. formulations thereof and their use in the treatment of anti-protozoal infections, especially malaria are described.
1,2,4-oxsdiuok 衍
生物:
其中 R1 是
氨基或取代
氨基;每个 R2 在 3、4、5 或 6 位中的一个或多个位置上相同或不同,并且是氢、低级烷基、卤素、羟基、烷氧基、烷
硫基、芳
硫基、
氨基、取代
氨基、
氰基或硝基:X和Y一起代表键或X和Y都是氢;R3是氢、低级烷基、芳基、取代芳基或ArS.
CH2-;Ar是未取代的或单取代的、二取代的或三取代的苯基,其中取代基可以相同或不同,本发明描述了其酸加成盐、其制备方法、其制剂及其在治疗抗原虫感染,特别是疟疾中的用途。