In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones

Six 7-benzylamino-1-isoquinolinamines 2 were found to be submicromolar inhibitors in vitro of drug-resistant Plasmodium falciparum, with the best possessing activity comparable to chloroquine. Despite being developed from a lead that is a DHFR inhibitor, these compounds do not mediate their antimala...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (2), p.786-789
Hauptverfasser:	Gutteridge, Clare E., Hoffman, Marshall M., Bhattacharjee, Apurba K., Milhous, Wilbur K., Gerena, Lucia
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminoquinolines - chemistry Aminoquinolines - pharmacology Antimalarials - chemistry Antimalarials - pharmacology Chalcone chalcones Chalcones - chemistry Chalcones - pharmacology chloroquine Chloroquine - chemistry Chloroquine - pharmacology Drug Resistance Humans In vitro efficacy Malaria Malaria, Falciparum - drug therapy Models, Molecular Plasmodium Plasmodium falciparum Plasmodium falciparum - drug effects Quinolinamine Structure-Activity Relationship
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