SYNTHESIS OF SOME 2, 6, 9-SUBSTITUTED THIOGUANINE ANDTHEIR ANTIMALARIAL ACTIVITY

In wide screening thioguanine has been shown to possess moderate activity against chloroquine resistant strain of Plasmodium berghei in mice. In order to search for new antimalarial agents superior to thioguanine, a series of 2,6,9-substituted thioguanines were prepared.Preliminary antimalarial tests revealed that 2-amino-6-S-propyl(n) thiopurine (compound 3) and 2-amino-6-(S-acetonyl) thiopurine (compound 5) were more active than thioguanine against chloroquine-resistant strain of P. berghei in mice.The pharmacological studies of these Compounds will be reported elsewhere.