Antimalarial activity of some novel derivatives of 2,4-diamino-5(p-chlorophenyl)-6-ethylpyrimidine (pyrimethamine).
Thirteen new analogs of 2,4-diamino-5(p-chlorophenyl)-6-ethylpyrimidine (Daraprim, pyrimethamine) in which the alph position of the 6-ethyl substituent was modified were prepared. The respective oxygens analogs (ketals, ketone, alcohol), the dimethyl hydrazone, and the nitrone displayed activities in the range of 1/4 to 1/16 that of pyrimethamine toward Plasmodium berghei in mice. The therapeutic ratios of some of these compounds may be slightly better than that of pyrimethamine.
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D002645:Chickens; D008288:Malaria / Q000188:drug therapy; D008289:Malaria, Avian / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei; D011739:Pyrimethamine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000962:Antimalarials; D011739:Pyrimethamine