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Published on: November 5, 2021
Enhanced Remdesivir Analogues to Target SARS-CoV-2
Ryuichi Majima1, Tiffany C Edwards1, Christine D Dreis1
1Center 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.
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