Antimalarial activity of 2,6-dibenzylidenecyclohexanone derivatives

[Display omitted] 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...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry letters 2021-09, Vol.47, p.128216-128216, Article 128216
Hauptverfasser: Eagon, Scott, Hammill, Jared T., Fitzsimmons, Kasey, Sienko, Natalie, Nguyen, Brandon, Law, Jarvis, Manjunath, Aashrita, Wilkinson, Steven P., Thompson, Kara, Glidden, Julia Elizabeth, Rice, Amy L., Falade, Mofolusho O., Kimball, Joshua J., DiBernardo, Celine, Guy, R. Kiplin
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2021.128216