J. F. Ryley
Dec 1, 1953
Citations
0
Influential Citations
23
Citations
Journal
British journal of pharmacology and chemotherapy
Abstract
During recent years considerable interest has been aroused by the ability of a number of substances to antagonize pteroylglutamic acid in both microbial and mammalian systems. Discussing the antagonistic effects of substituted 2: 4-diaminopyrimidines, Falco,. Hitchings, Russell, and VanderWerff (1949) pointed out that these substances showed a formal resemblance to proguanil (" Paludrine "), and might therefore be expected to have antimalarial activity also. They suggested, too, that by virtue of this similarity proguanil should display pterolyglutamic acid antagonism in their bacterial cultures. Development of the idea that 2: 4-diaminopyrimidines might possess antimalarial activity led to the synthesis of pyrimethamine (2: 4-diamino-5-p-chlorophenyl-6ethylpyrimidine; " Daraprim "), one of the most active compounds of the series, as an antimalarial drug.