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

Bioorg Med Chem Lett. 2021 Sep 1:47:128196. doi: 10.1016/j.bmcl.2021.128196.

Alexis Pinet ¹, Sandrine Cojean ², Linh Thuy Nguyen ³, Pedro Vásquez-Ocmín ¹, Alexandre Maciuk ¹, Philippe M Loiseau ¹, Patrice Le Pape ⁴, Bruno Figadère ¹, Laurent Ferrié ⁵

Affiliations

1 BioCIS, CNRS, Université Paris-Saclay, Châtenay-Malabry 92290, France.
2 BioCIS, CNRS, Université Paris-Saclay, Châtenay-Malabry 92290, France; National de Référence du Paludisme, Hôpital Bichat-Claude Bernard, APHP, 75018 Paris, France.
3 BioCIS, CNRS, Université Paris-Saclay, Châtenay-Malabry 92290, France; Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), Cau Giay, Hanoi, Viet Nam.
4 Department of Parasitology and Medical Mycology University of Nantes, EA1155 IICiMed, Nantes Atlantique Universities, Faculty of Pharmacy, Nantes, France.
5 BioCIS, CNRS, Université Paris-Saclay, Châtenay-Malabry 92290, France. Electronic address: [email protected].

PMID: 34116159 DOI: 10.1016/j.bmcl.2021.128196

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.

Keywords

1,2-Dioxolane; Antifungal; Antileishmanial; Antimalarial; Endoperoxide.

Name
Email *

	Sorry, but the email address you supplied was invalid.