[Synthesis and antiprotozoal activity of [1,3]oxazino[4,5,6-de]quinolines].
The synthesis of 1,3-oxazino-anellated 4-amino-5-hydroxy-quinolines has been investigated. Cyclisation to 2,3-dihydro[1,3]oxazino[4,5,6-de]quinoline-2-ones/-2-thiones (2/3) was achieved by reaction with 1,1'-carbonyldiimidazole or 1,1'-thiocarbonyldiimidazole. Cyclocondensation with aldehydes yielded 2,3-dihydro[1,3]oxazino[4,5,6-de]quinoline-derivatives (5). All new tricyclic compounds exhibited weak antiprotozoal activity against Plasmodium falciparum.
Meyer
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Institut für Pharmazie, Universität Hamburg, Germany.
Geffken
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D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D003500:Cyclization; D004912:Erythrocytes / Q000469:parasitology; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D010963:Plasmodium falciparum / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
D000962:Antimalarials; D007202:Indicators and Reagents; D011804:Quinolines
Synthese und antiplasmodiale Wirksamkeit von [1,3]Oxazino[4,5,6-de]chinolinen.