Antimalarials. 10. Substituted 3-halo- and 3-methoxy-2-aryl-4-quinoline(di-n-butylaminomethyl)methanols.
Four 2-aryl-4-quinoline(di-n-butylaminomethyl)methanols with Br, Cl, F, or OMe in position 3 were synthesized by modifications of standard reactions. The antimalarial activity decreased with increased size of the 3-substituent. The 3-F-4',6,8-Cl3 compound was the most active (at 2.5 mg/kg) and was completely curative at 80 mg/kg against P. berghei in mice.
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D008288:Malaria / Q000188:drug therapy; D000432:Methanol / Q000138:chemical synthesis / Q000627:therapeutic use; D051379:Mice; D010962:Plasmodium berghei; D011804:Quinolines / Q000138:chemical synthesis* / Q000627:therapeutic use
D000962:Antimalarials; D011804:Quinolines; D000432:Methanol