Reduced 8-aminoquinoline analogues as potential antimalarial agents.
The synthesis of 1-alkyl-8-(aminoalkylamino)-6-methyl1-1,2,3,4-tetrahydroquinolines, 8-(4'-amino-1'-methylbutylamino)-6-methoxy-1-methyl1-1,2-dihydroquinoline, 5-substituted 8-(4'-amino-1'-methylbutylamino)-1-methyl-1,2-dihydroquinolines, 8-alkylamino-1-(2-N,N-diethylaminoethyl)-6-methoxy-1,2,3,4-tetrahydroquinolines, 1-)2-N,N-diethylaminoethyl)-6-methoxy-1,2,3,4-tetrahydroquinoline, 1-(2-N,N-diethylaminoethyl)-8-(2-N,N-diethylaminoethylamino)-6-methoxy-1,2,3,4-tetrahydroquinoline, and 2-substituted 8-methoxy-5,6,-dihydro-4-imidazo [i,j]quinolines is described. These compounds as well as most of the intermediates used in their preparation were tested against Plasmodium berghei in mice, and a few compounds were tested for prophylactic activity against Plasmodium cynomolgi in rhesus monkeys.
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000627:therapeutic use; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D000882:Haplorhini; D008253:Macaca mulatta; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei; D013329:Structure-Activity Relationship
D000634:Aminoquinolines; D000962:Antimalarials