Elslager E F, Johnson J L, Werbel L M
J Med Chem. 1981 Aug;24(8):1001-3. doi: 10.1021/jm00140a017.
A series of 6-(arylthio)-2,4-pteridinediamines (IIIa) was prepared by allowing 6-chloro-2,4-pteridinediamine to react with the requisite benzenethiols in dimethyl sulfone at 190-200 degrees C. Attempts at oxidation to the corresponding sulfoxide (IIIb) or sulfone (IIIc) were unsuccessful. The compounds exhibited a spectrum of antibacterial activity similar to, but below the potency of, the related quinazolinediamines and pteridinediamines. Unlike these related types, however, they were devoid of antimalarial activity when tested against a normal drug-sensitive strain of Plasmodium berghei in mice by the parenteral route.
通过使6-氯-2,4-蝶啶二胺与所需的苯硫酚在190 - 200℃的二甲基砜中反应，制备了一系列6-(芳硫基)-2,4-蝶啶二胺(IIIa)。将其氧化为相应的亚砜(IIIb)或砜(IIIc)的尝试未成功。这些化合物表现出的抗菌活性谱与相关的喹唑啉二胺和蝶啶二胺相似，但效力低于它们。然而，与这些相关类型不同的是，当通过非肠道途径在小鼠中针对正常的对药物敏感的伯氏疟原虫菌株进行测试时，它们没有抗疟活性。
