[Antimalarial 6-aminoquinolines. XI. 2-, 3-, and 4-alkyl-, aryl-, and arylalkyl derivatives (author's transl)].
23 derivatives 17a--z of 6-(4-diethylamino-1-methylbutylamino)-5,8-dimethoxyquinoline (1a) were synthesized with the aim of studying the influence of an increased lipophilicity on the biological activity. 17a--z are active against P. vinckei (mouse), but none of these derivatives is superior to the 2,4-dimethyl derivative 1d. Flat molecules (e.g. 17k and 17e) and their bulky hydrogenated derivatives (17I and 17f) show a comparable activity. This indicates that a flat structure is not essential for the activity of the 6-aminoquinolines.
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D008288:Malaria / Q000188:drug therapy; D008722:Methods; D051379:Mice; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D000634:Aminoquinolines; D000962:Antimalarials
Gegen Malaria wirksame 6-Aminochinoline. XI. 2-, 3-, und 4-Alkyl-, Aryl- und Arylalkylderivate.