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Updated: Apr 28, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
1,4-naphthoquinone cations as antiplasmodial agents: hydroxy-, acyloxy-, and alkoxy-substituted analogues
Xiao Lu1, Ali Altharawi1, Jiri Gut2
1Department of Pharmaceutical and Biomedical Sciences, University of Georgia , Athens, Georgia 30602, United States.
Abstract:
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.
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