4.5 Article

Antimalarial activity of 2,6-dibenzylidenecyclohexanone derivatives

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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

  1. Bill and Linda Frost Fund at Cali-fornia Polytechnic State University

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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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