Topological and Multivalent Effects in Glycofullerene Oligomers as EBOLA Virus Inhibitors

Impacto

Downloads

Downloads per month over past year

Ramos Soriano, Javier and Illescas, Beatriz M. and Pérez Sánchez, Alfonso and Sánchez Bento, Raquel and Lasala, Fátima and Rojo, Javier and Delgado Vázquez, Rafael and Martín, Nazario (2022) Topological and Multivalent Effects in Glycofullerene Oligomers as EBOLA Virus Inhibitors. International Journal of Molecular Sciences, 23 (9). p. 5083. ISSN 1422-0067

[thumbnail of ijms-23-05083-v3.pdf]
Preview
PDF
Creative Commons Attribution.

2MB

Official URL: https://doi.org/10.3390/ijms23095083




Abstract

The synthesis of new biocompatible antiviral materials to fight against the development of multidrug resistance is being widely explored. Due to their unique globular structure and excellent properties, [60]fullerene-based antivirals are very promising bioconjugates. In this work, fullerene derivatives with different topologies and number of glycofullerene units were synthesized by using a SPAAC copper free strategy. This procedure allowed the synthesis of compounds 1–3, containing from 20 to 40 mannose units, in a very efficient manner and in short reaction times under MW irradiation. The glycoderivatives were studied in an infection assay by a pseudotyped viral particle with Ebola virus GP1. The results obtained show that these glycofullerene oligomers are efficient inhibitors of EBOV infection with IC50s in the nanomolar range. In particular, compound 3, with four glycofullerene moieties, presents an outstanding relative inhibitory potency (RIP). We propose that this high RIP value stems from the appropriate topological features that efficiently interact with DC-SIGN.


Item Type:Article
Uncontrolled Keywords:glycofullerene; click chemistry; Ebola virus; antivirals; DC-SIGN
Subjects:Medical sciences > Medicine > Immunology
ID Code:74832
Deposited On:06 Oct 2022 13:34
Last Modified:07 Oct 2022 07:35

Origin of downloads

Repository Staff Only: item control page