Deoxythymidine derivatives according to formula (I) are disclosed. wherein: X may be O or S; and R1, R2, R3, R4 and R5 may each be independently selected from H, halo, C1-C6 alkyl, C1-C6 haloalkyl, nitro, phenyl, heteroaryl, substituted heteroaryl wherein the substituents may be C1-C6 alkyl or C1-C6 haloalkyl, benzyl, -CH2OAr, -OR6 and six-membered ring heterocyclic groups containing 1 or more O and/or N heteroatoms wherein any N heteroatom may be C1-C6 alkyl-substituted; and R6 may be selected from C1-C6 alkyl, phenyl, six-membered ring heterocyclic groups containing at least one O heteroatom, benzyl and substituted benzyl wherein the substituents may be halo, C1-C6 alkyl or C1-C6 alkoxy; R7 may be H or C1-C6 alkyl; and the stereochemistry of the bond depicted as 〰 is either α or β. Such derivatives have shown good inhibitory activity against malaria-causing parasites, e.g. Plasmodium falciparum, but have shown low levels of toxicity to human cells.
根据公式(I),披露了
脱氧胸苷衍
生物。其中:X可以是O或S;R1、R2、R3、R4和R5可以分别独立地选择自H、卤素、C1-C6烷基、C1-C6卤代烷基、硝基、
苯基、杂环芳基、取代的杂环芳基,其中取代基可以是C1-C6烷基或C1-C6卤代烷基、
苄基、-
CH2OAr、-OR6和含有1个或多个O和/或N杂原子的六元环杂环基团,其中任何N杂原子可以是C1-C6烷基取代的;R6可以选择自C1-C6烷基、
苯基、含有至少一个O杂原子的六元环杂环基团、
苄基和取代的
苄基,其中取代基可以是卤素、C1-C6烷基或C1-C6烷
氧基;R7可以是H或C1-C6烷基;而所示键的立体
化学为α或β。这些衍
生物已显示出对引起疟疾的寄生虫,如疟原虫(Plasmodium falciparum),具有良好的抑制活性,但对人类细胞的毒性
水平较低。