4,5-Disubstituted primaquine analogues as potential antimalarial agents

Three 4,5-disubstituted primaquine analogues were synthesized and evaluated for radical curative activity against Plasmodium cynomolgi in rhesus monkeys. One of the compounds showed moderate activity; however, none of the three compounds were as active as the lead compounds 5-methoxy-4-methylprimaqu...

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Veröffentlicht in:	Journal of medicinal chemistry 1986-09, Vol.29 (9), p.1796-1798
Hauptverfasser:	Carroll, F. Ivy, Berrang, Bertold D, Linn, Carl P
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Chemical Phenomena Chemistry Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with only one n hetero atom and condensed derivatives Macaca mulatta Malaria - drug therapy Organic chemistry Preparations and properties Primaquine - analogs & derivatives Primaquine - therapeutic use Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	Three 4,5-disubstituted primaquine analogues were synthesized and evaluated for radical curative activity against Plasmodium cynomolgi in rhesus monkeys. One of the compounds showed moderate activity; however, none of the three compounds were as active as the lead compounds 5-methoxy-4-methylprimaquine and 4-(methoxy-methyl)-5-[m-(trifluoromethyl)phenoxy]primaquine.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00159a042