Anti-protozoal and anti-fungal evaluation of 3,5-disubstituted 1,2-dioxolanes

[Display omitted] •Biological evaluation of 3,5-disubstituted 1,2-dioxolanes was for the first time reported.•Compounds 5a and 10c showed excellent antimalarial activity.•Compounds 8c, 9c, 15c and 16c displayed potential antileishmanial activities. Endoperoxides are a class of compounds, which is we...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2021-09, Vol.47, p.128196-128196, Article 128196
Hauptverfasser: Pinet, Alexis, Cojean, Sandrine, Nguyen, Linh Thuy, Vásquez-Ocmín, Pedro, Maciuk, Alexandre, Loiseau, Philippe M., Le Pape, Patrice, Figadère, Bruno, Ferrié, Laurent
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Sprache:eng
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Zusammenfassung:[Display omitted] •Biological evaluation of 3,5-disubstituted 1,2-dioxolanes was for the first time reported.•Compounds 5a and 10c showed excellent antimalarial activity.•Compounds 8c, 9c, 15c and 16c displayed potential antileishmanial activities. Endoperoxides are a class of compounds, which is well-known for their antimalarial properties, but few reports exist about 3,5-disubstituted 1,2-dioxolanes. After having designed a new synthetic route for the preparation of these substances, they were evaluated against 4 different agents of infectious diseases, protozoa (Plasmodium and Leishmania) and Fungi (Candida and Aspergillus). Whereas moderate antifungal activity was found for our products, potent antimalarial and antileishmanial activities were observed for a few compounds. The nature of the substituents linked to the endoperoxide ring seems to play an important role in the bioactivities.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2021.128196