22272-18-0Relevant articles and documents
Synthetic schistosomicides. XIV. 1,4-naphthoquinone mono(O-acyloximes), 4-amino-1,2-naphthoquinones, 2-amino-3-chloro-1,4-naphthoquinones, and other naphthoquinones.
Elslager,Werbel,Worth
, p. 104 - 109 (1970)
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Antimalarial N1, N3-Dialkyldioxonaphthoimidazoliums: Synthesis, Biological Activity, and Structure-activity Relationships
Ahenkorah, Stephen,Birkholtz, Lyn-Marie,Coertzen, Dina,Fridianto, Kevin,Go, Mei-Lin,Haynes, Richard K.,Lam, Yulin,Tan, Kevin S. W.,Tong, Jie Xin,Wittlin, Sergio
supporting information, p. 49 - 55 (2020/02/06)
Here we report the nanomolar potencies of N1,N3-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.