Synthesis of 2,4-disubstituted 6-methoxy-8-aminoquinoline analogues as potential antiparasitics.
A series of 2,4-disubstituted 8-aminoquinoline analogues were synthesized and evaluated against Plasmodium berghei in mice and Leishmania donovani in hamsters. 8-[[6-(Diethylamino)hexyl]amino]-2-ethyl-6-methoxy-4-methylquinoline (8a) possessed significant activity against L. donovani. 2-Ethyl-4-methylprimaquine (7a) was evaluated against Plasmodium cynomolgi in rhesus monkey and found to have activity equal to that of primaquine.
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis; D000981:Antiprotozoal Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D000882:Haplorhini; D007891:Leishmania / Q000187:drug effects; D008253:Macaca mulatta; D008288:Malaria / Q000188:drug therapy; D010961:Plasmodium / Q000187:drug effects
D000634:Aminoquinolines; D000962:Antimalarials; D000981:Antiprotozoal Agents