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8-Aminoquinolines: Primaquine and Tafenoquine
20118-Aminoquinolines are an important class of antimalarial drugs because they are effective against the liver stages of Plasmodium infections and thus are administered for radical cure and presumptive antirelapse therapy against relapsing malaria. In this chapter, we discuss two 8-aminoquinolines, primaquine and tafenoquine.
Norman C. Waters, Michael D. Edstein
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Synthesis of aminals from 8-aminoquinoline
Chemistry of Heterocyclic Compounds, 1981The reaction of 8-aminoquinoline with substituted aromatic aldehydes leads to aminals, which are the only reaction products. The reaction with 1-formyl-2-hydroxynaphthalene proceeds with the formation of a Schiff base. The UV and mass spectra of the aminals are discussed.
N. S. Kozlov, G. V. Vorob'eva
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Reduced 8-aminoquinoline analogues as potential antimalarial agents
Journal of Medicinal Chemistry, 1976The 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 ...
F I, Carroll +3 more
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Tafenoquine: A New 8- Aminoquinoline
Medical Journal of Zambia, 2012No ...
Prashar, L, Paul, R
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Copper-Catalyzed Regioselective C–H Sulfonylation of 8-Aminoquinolines
The Journal of Organic Chemistry, 2016Copper(I)-catalyzed 5-sulfonation of quinolines via bidentate-chelation assistance has been developed. The reaction is compatible with a wide range of quinoline substrates and arylsulfonyl chlorides. Experimental and theoretical (DFT) investigation implicated that a single-electron-transfer process is involved in this sulfonylation transformation.
Jun, Wei +7 more
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Antimalarial Activity of Novel 5-Aryl-8-Aminoquinoline Derivatives
Journal of Medicinal Chemistry, 2010In an attempt to separate the antimalarial activity of tafenoquine (3) from its hemolytic side effects in glucose-6-phosphate dehydrogenase (G6PD) deficiency patients, a series of 5-aryl-8-aminoquinoline derivatives was prepared and assessed for antimalarial activities.
Hiroaki, Shiraki +6 more
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8-Aminoquinolines as anticoccidials-I
Bioorganic & Medicinal Chemistry Letters, 1997Richard E. Armer +6 more
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Derivatives of 6-Methoxy-8-aminoquinoline and 2-Methyl-6-methoxy-8-aminoquinoline. II
Journal of the American Chemical Society, 1944Ewald Rohrmann, H. A. Shonle
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