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.
|Journal||Bioorganic and Medicinal Chemistry Letters|
|State||Published - Sep 1 2021|
Bibliographical noteFunding Information:
This work was supported by the Bill and Linda Frost Fund at California Polytechnic State University (no associated grant number).
© 2021 The Author(s)
- Michael system
- Plasmodium falciparum
- Structure activity relationship
ASJC Scopus subject areas
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry