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ID: ALA4334542
Journal: ACS Med Chem Lett
Title: Antimalarial N 1,N 3-Dialkyldioxonaphthoimidazoliums: Synthesis, Biological Activity, and Structure-activity Relationships.
Authors: Ahenkorah S, Coertzen D, Tong JX, Fridianto K, Wittlin S, Birkholtz LM, Tan KSW, Lam Y, Go ML, Haynes RK.
Abstract: Here we report the nanomolar potencies of N 1,N 3-dialkyldioxonaphthoimidazoliums against asexual forms of sensitive and resistant Plasmodium falciparum. Activity was dependent on the presence of the fused quinone-imidazolium entity and lipophilicity imparted by the N1/N3 alkyl residues on the scaffold. Gametocytocidal activity was also detected, with most members active at IC50 < 1 μM. A representative analog with good solubility, limited PAMPA permeability, and microsomal stability demonstrated oral efficacy on a humanized mouse model of P. falciparum.
CiteXplore: 31938463