Antimalarials. 11. Synthesis of 3- and 5-aminoquinolines as potential antimalarials.
A series of 3-quinolinediamines (1g, 2c, and 3e) structurally related to primaquine and 4-methylprimaquine have been prepared and tested for antimalarial activity against Plasmodium berghei in mice and antileishmanial activity against Leishmania donovani in the hamster. All were inactive. In addition, three 5-quinolinediamines (4b, 5, and 6) were prepared. All were inactive against Leishmania donovani in hamsters. One of the examples, 6, was curative against Plasmodium cynmolgi in the rhesus monkey.
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D006224:Cricetinae; D000882:Haplorhini; D007891:Leishmania; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei
D000634:Aminoquinolines; D000962:Antimalarials