Optimization of endochin-like quinolones for antimalarial activity

Structural analogs of the antimalarial endochin were synthesized and screened for antiplasmodial activity against drug sensitive and multidrug resistant strains of Plasmodium falciparum. Structural features have been identified that are associated with improved potency while other features are assoc...

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Veröffentlicht in:	Experimental parasitology 2011-02, Vol.127 (2), p.545-551
Hauptverfasser:	Winter, Rolf, Kelly, Jane X., Smilkstein, Martin J., Hinrichs, David, Koop, Dennis R., Riscoe, Michael K.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals antimalarials Antimalarials - chemistry Antimalarials - pharmacology Antimalarials - therapeutic use Biological and medical sciences Chemotherapy Cytochrome bc1 complex Disease Models, Animal Drug resistance Drug Stability Electron transport chain Female Fundamental and applied biological sciences. Psychology Human protozoal diseases Humans Infectious diseases Inhibitors Life cycle. Host-agent relationship. Pathogenesis Malaria Malaria - drug therapy Medical sciences Mice microsomes Microsomes, Liver - metabolism multiple drug resistance oral administration Parasitic diseases parasitology Plasmodium falciparum Plasmodium falciparum - drug effects Plasmodium yoelii Plasmodium yoelii - drug effects polyethylene glycol Prodrug Protozoa Protozoal diseases quinolones Quinolones - chemistry Quinolones - pharmacology Quinolones - therapeutic use Rats Structure-Activity Relationship structure-activity relationships therapeutics
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