Work

1,4-Naphthoquinone Cations as Antiplasmodial Agents: Hydroxy-, Acyloxy-, and Alkoxy-Substituted Analogues

Year: 2012

Type: article

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.

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/ml300242v

Authors: Xiao Lu, Ali Altharawi, Jiri Gut, Philip J. Rosenthal, Timothy E. Long

Institutions: University of Georgia, San Francisco General Hospital, University of California, San Francisco

Language: English

Topic: Malaria Research and Control

Subfield: Public Health, Environmental and Occupational Health

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: green

Funders: Doris Duke Charitable Foundation, University of Georgia, National Institutes of Health