Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides

Article abstract of DOI:10.1021/jm00378a038

The synthesis and antimalarial activity of a series of 2,4-diamino-6-quinazolinesulfonamides is described. Chlorosulfonation of 2,4-quinazolinediamine affords the 6-sulfonyl chloride, which upon treatment with the appropriate amine produces the desired products. Alternatively the sulfonyl chloride could be introduced by diazotization of the corresponding amine followed by treatment with SO₂ in the presence of CuCl₂. Although substantial antimalarial activity was demonstrated for several members of this class, studies were discontinued in light of the potency of related series.