Modifications of primaquine as antimalarials. 4. 5-Alkoxy derivatives of primaquine

Modifications of primaquine as antimalarials. 4. 5-Alkoxy derivatives of primaquine

Thirty-two 5-alkoxyprimaquines have been synthesized and evaluated as blood schizonticides (Plasmodium berghei, mouse) and tissue schizonticides (Plasmodium cynomolgi, monkey). Several of these compounds were extremely active in both screens. Such a broad spectrum of antimalarial efficacy offers the...

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Veröffentlicht in:Journal of medicinal chemistry 1987-07, Vol.30 (7), p.1193-1199
Hauptverfasser: Chen, Eugene H, Tanabe, Keiichi, Saggiomo, Andrew J, Nodiff, Edward A
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Antimalarials - chemical synthesis
Antimalarials - pharmacology
Malaria - drug therapy
Mice
Primaquine - analogs & derivatives
Structure-Activity Relationship
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Zusammenfassung:Thirty-two 5-alkoxyprimaquines have been synthesized and evaluated as blood schizonticides (Plasmodium berghei, mouse) and tissue schizonticides (Plasmodium cynomolgi, monkey). Several of these compounds were extremely active in both screens. Such a broad spectrum of antimalarial efficacy offers the possibility of a single drug that could cure the various relapsing and nonrelapsing malarias.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00390a012