Malaria Box-Inspired Discovery of N-Aminoalkyl-β-carboline-3-carboxamides, a Novel Orally Active Class of Antimalarials.
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DOI: 10.1021/acsmedchemlett.1c00663
Abstract: Virtual ligand screening of a publicly available database of antimalarial hits using a pharmacophore derived from antimalarial MMV008138 identified TCMDC-140230, a tetrahydro-β-carboline amide, as worthy of exploration. All four stereoisomers of this structure were synthesized,… read more here.
Keywords: carboline; discovery aminoalkyl; aminoalkyl carboline; box inspired ... See more keywords
Malaria Box Compounds against Anopheles gambiae (Diptera: Culicidae) Carboxypeptidase B Activity to Block Malaria Transmission
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DOI: 10.1093/jme/tjac043
Abstract: Abstract Carboxypeptidase B (CPB) plays an important role in blood digestion in mosquitos, aiding the release of free amino acids. Anopheles CPB is a target to block malaria transmission because it facilitates Plasmodium invasion of… read more here.
Keywords: activity; box compounds; malaria box; malaria ... See more keywords
Antiplasmodial profile of selected compounds from Malaria Box: in vitro evaluation, speed of action and drug combination studies
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DOI: 10.1186/s12936-019-3069-3
Abstract: BackgroundArtemisinin-based combination therapy (ACT) is used as the first-line treatment of uncomplicated malaria caused by the Plasmodium falciparum parasite and chloroquine-resistant Plasmodium vivax parasites. Evidence of resistance to ACT has been reported in Cambodia, and… read more here.
Keywords: combination; malaria box; speed action; activity ... See more keywords
New Derivatives of the Multi-Stage Active Malaria Box Compound MMV030666 and Their Antiplasmodial Potencies
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DOI: 10.3390/ph15121503
Abstract: MMV’s Malaria Box compound MMV030666 shows multi-stage activity against various strains of Plasmodium falciparum and lacks resistance development. To evaluate the importance of its diarylether partial structure, diarylthioethers and diphenylamines with varying substitution patterns were… read more here.
Keywords: compound; box compound; compound mmv030666; multi stage ... See more keywords