Electrochemical oxidation of 5-hydroxymethylfurfural (HMF) is a promising synthetic route for 2,5-furandicarboxylic acid (FDCA) production. Here, we prepared a nickel(II)-modified covalent-organic framework (COF) film TpBpy-Ni@FTO for HMF electrooxidation. With a...
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, but none
potently inhibited growth of the malaria parasite Plasmodium
falciparum. Interestingly, 7e, a minor byproduct
of these syntheses, proved to be potent in vitro against P. falciparum and was orally efficacious (40 mg/kg) in an in vivo mouse model of malaria.
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