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

Abstract

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-1isolates 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.