1402665-84-2Relevant academic research and scientific papers
SMALL MOLECULE NAPHTHOQUINONE- AND PHTHALIMIDE-BASED LIPOCATIONS AS ANTI-PARASITIC AGENTS
-
Page/Page column 48; 50, (2013/03/26)
Small molecule naphthoquinone- and phthalimide-based lipocations are provided, as well as methods for their use in treating or preventing anti-parasitic diseases, such as malaria, Chagas disease, and African Sleeping Sickness.
1,4-naphthoquinone cations as antiplasmodial agents: Hydroxy-, acyloxy-, and alkoxy-substituted analogues
Lu, Xiao,Altharawi, Ali,Gut, Jiri,Rosenthal, Philip J.,Long, Timothy E.
, p. 1029 - 1033 (2013/02/22)
Cations of hydroxy-substituted 1,4-naphthoquinones were synthesized and evaluated as antiplasmodial agents against Plasmodium falciparum. The atovaquone analogues were found to be inactive as antagonists of parasite growth, which was attributed to ionization of the acidic hydroxyl moiety. Upon modification to an alkoxy substituent, the antiplasmodial activity was restored in the sub-100 nM range. Optimal inhibitors were found to possess IC50 values of 17.4-49.5 nM against heteroresistant P. falciparum W2.
