Folate antagonists. 19. Synthesis and antimalarial effects of 6-(arylthio)-2,4-pteridinediamines.

  title={Folate antagonists. 19. Synthesis and antimalarial effects of 6-(arylthio)-2,4-pteridinediamines.},
  author={Edward F. Elslager and Joyce Johnson and Leslie Morton Werbel},
  journal={Journal of medicinal chemistry},
  volume={24 8},
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… CONTINUE READING

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