Chemical Biology & Drug Design · 2022 · 10 citations · 21 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoverySynthetic Medicinal ChemistryChemical Library DesignEnzyme InhibitionHit-to-lead OptimizationLead Compound DesignLigand-based DesignStructure-activity Relationship AnalysisAntimalarial Drug DevelopmentChemotherapy Of MalariaHeterocyclic LigandsMechanistic ElucidationPlasmodium FalciparumQuinoline ChemistryQuinoline SynthesisTreatment Of Malaria
Abstract A library of quinoline‐based hydrazones bearing 1 H ‐1,2,3‐triazole core was designed, synthesized, and evaluated for their antiplasmodial activity against the drug‐resistant Plasmodium falciparum W2 strain. The inclusion of pyrazine‐2‐carboxylic acid with a flexible propyl spacer afforded the most active scaffold with an IC 50 value of 0.26 μM. Mechanistically, the compound inhibited heme to hemozoin formation, as demonstrated by UV–vis and mass spectral studies.
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Timothy J. Egan, Roger Hunter, Catherine H. Kaschula et al. · Journal of Medicinal Chemistry · 1999 · 311 citations
Sandra Gemma, Gagan Kukreja, Caterina Fattorusso et al. · Bioorganic & Medicinal Chemistry Letters · 2006 · 158 citations · Full text