Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
The synthesis and antimalarial activity of a series of 2,4,6-triaminopyrido[3,2-d]pyrimidines (4) is described. Several 6-substituted benzylmethylamino analogues were more active against trophozoite induced Plasmodium berghei in mice than the corresponding quinazoline analogues. These agents, however, are cross-resistant to other antifolate compounds and are thus of limited potential as human agents.
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis*; D004351:Drug Resistance; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000962:Antimalarials; D011743:Pyrimidines