[Antimalarial 10 H-indolo(3,2-b)quinolin-11-yl-amines. 1. Phenol-Mannich-bases of the amodiaquine and cycloquine type].
The 11-chloro-quinoline derivatives 3 react with 4-aminophenol and the mono- and bis-phenol-Mannich-bases 6 to yield the 10H-indolo[3,2-b]quinoline-11-yl-amines 4 and 7. The amodiaquine analogue 7a as the best of all compounds shows a comparable activity with choroquine and inhibits a multiresistant Plasmodium falciparum strain at the same concentration. Compound 7e from the cycloquine-type was selected for an in vivo antitumor screening programme.
Görlitzer
K
K
Institut für Pharmazeutische Chemie, Technischen Universität Braunschweig.
Stockmann
R
R
Walter
R D
RD
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D000998:Antiviral Agents / Q000494:pharmacology; D004351:Drug Resistance; D004354:Drug Screening Assays, Antitumor; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects
D000634:Aminoquinolines; D000962:Antimalarials; D000998:Antiviral Agents; D007211:Indoles
Gegen Malaria wirksame 10H-Indolo[3,2-b]chinolin-11-yl-amine. 1. Mitteilung: Phenol-Mannich-Basen vom Amodiaquin- und Cycloquin-Typ.