Potential antimalarials. XXII Some 2,4-diamino-5-(3- and 4-trifluoromethylphenyl and 3,4-methylenedioxyphenyl)pyrimidines

Article abstract of DOI:10.1071/ch9960647

A series of 10 pyrimethamine analogues containing 3′- and 4′-trifluoromethyl and 3′,4′-methylenedioxy groups has been prepared and tested for in vitro antimalarial activity against the FC-27 and K-1 isolates of Plasmodium falciparum. Several of these compounds were almost as active as pyrimethamine against the drug-sensitive FC-27 isolate, and like pyrimethamine, they were much less active against the drug-resistant K-1 isolate. The 4′-trifluoromethyl compunds, however, showed much smaller differences.