Enhanced Remdesivir Analogues to Target SARS-CoV-2

Ryuichi Majima; Tiffany C. Edwards; Christine D. Dreis; Robert J. Geraghty; Laurent F. Bonnac

doi:10.3390/molecules28062616

Enhanced Remdesivir Analogues to Target SARS-CoV-2

Ryuichi Majima, Tiffany C. Edwards, Christine D. Dreis, Robert J. Geraghty, Laurent F. Bonnac

Center for Drug Design

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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.

Original language	English (US)
Article number	2616
Journal	Molecules
Volume	28
Issue number	6
DOIs	https://doi.org/10.3390/molecules28062616
State	Published - Mar 2023

Bibliographical note

Publisher Copyright:
© 2023 by the authors.

Keywords

C-nucleoside
SARS-CoV-2
antiviral
phosphate prodrug

PubMed: MeSH publication types

Journal Article

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AU - Dreis, Christine D.

AU - Geraghty, Robert J.

AU - Bonnac, Laurent F.

PY - 2023/3

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AB - 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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KW - SARS-CoV-2

KW - antiviral

KW - phosphate prodrug

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Enhanced Remdesivir Analogues to Target SARS-CoV-2

Abstract

Bibliographical note

Keywords

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UN SDGs

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