Title
Anti-protozoal and anti-fungal evaluation of 3,5-disubstituted 1,2-dioxolanes
Date Issued
01 September 2021
Access level
open access
Resource Type
journal article
Author(s)
Pinet A.
Cojean S.
Nguyen L.T.
Maciuk A.
Loiseau P.M.
Le Pape P.
Figadère B.
Ferrié L.
Université Paris-Saclay
Publisher(s)
Elsevier Ltd
Abstract
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.
Volume
47
Language
English
OCDE Knowledge area
Enfermedades infecciosas
Parasitología
Farmacología, Farmacia
Subjects
Scopus EID
2-s2.0-85107769963
PubMed ID
Source
Bioorganic and Medicinal Chemistry Letters
ISSN of the container
0960894X
Sponsor(s)
A. Pinet thanks the Ministère de l’Enseignement Supérieur de la Recherche et de l’Innovation (MESRI) for a PhD fellowship. L. T. Nguyen thanks the Vietnamese government for a PhD fellowship. We thank Karine Leblanc for HRMS analysis (BioCIS, Châtenay-Malabry), Jean-Christophe Jullian (BioCIS, Châtenay-Malabry) for NMR services and Carine Picot for antifungal tests (EA1155 IICiMed).
Sources of information:
Directorio de Producción Científica
Scopus