期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 47, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128216
关键词
Malaria; Plasmodium falciparum; Structure activity relationship; Michael system; 2; 6-Dibenzylidenecyclohexanone
资金
- Bill and Linda Frost Fund at Cali-fornia Polytechnic State University
In the search for new anti-malarial drugs, this study reports the discovery of a derivative with potential efficacy against Plasmodium falciparum but without detectable toxicity.
Malaria remains one of the deadliest infectious diseases worldwide and continues to infect hundreds of millions of individuals each year. Here we report the discovery and derivatization of a series of 2,6-dibenzylidenecyclohexanones targeting the chloroquine-sensitive 3D7 strain of Plasmodium falciparum . While the initial lead compound displayed significant toxicity in a human cell proliferation assay, we were able to identify a derivative with no detectable toxicity and sub-micromolar potency.
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