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Matches in SemOpenAlex for { <https://semopenalex.org/work/W2015251548> ?p ?o ?g. }

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• W2015251548 abstract "The antiplasmodial activity of a series of spirotetrahydro beta-carbolines is described. Racemic spiroazepineindole (1) was identified from a phenotypic screen on wild type Plasmodium falciparum with an in vitro IC(50) of 90 nM. Structure-activity relationships for the optimization of 1 to compound 20a (IC(50) = 0.2 nM) including the identification of the active 1R,3S enantiomer and elimination of metabolic liabilities is presented. Improvement of the pharmacokinetic profile of the series translated to exceptional oral efficacy in the P. berghei infected malaria mouse model where full cure was achieved in four of five mice with three daily doses of 30 mg/kg." @default.
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• W2015251548 date "2010-06-22" @default.
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• W2015251548 title "Spirotetrahydro β-Carbolines (Spiroindolones): A New Class of Potent and Orally Efficacious Compounds for the Treatment of Malaria" @default.
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• W2015251548 doi "https://doi.org/10.1021/jm100410f" @default.
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