Enhanced Remdesivir Analogues to Target SARS-CoV-2

Author:

Majima Ryuichi1ORCID,Edwards Tiffany C.1,Dreis Christine D.1ORCID,Geraghty Robert J.1ORCID,Bonnac Laurent F.1ORCID

Affiliation:

1. Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA

Abstract

We report the short synthesis of novel C-nucleoside Remdesivir analogues, their cytotoxicity and an in vitro evaluation against SARS-CoV-2 (CoV2). The described compounds are nucleoside analogues bearing a nitrogen heterocycle as purine analogues. The hybrid structures described herein are designed to enhance the anti-CoV2 activity of Remdesivir. The compounds were evaluated for their cytotoxicity and their anti-CoV2 effect. We discuss the impact of combining both sugar and base modifications on the biological activities of these compounds, their lack of cytotoxicity and their antiviral efficacy.

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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