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

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

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

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Publisher Copyright:
© 2023 by the authors.

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This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

C-nucleoside
SARS-CoV-2
antiviral
phosphate prodrug

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10.3390/molecules28062616

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title = "Enhanced Remdesivir Analogues to Target SARS-CoV-2",

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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author = "Ryuichi Majima and Edwards, \{Tiffany C.\} and Dreis, \{Christine D.\} and Geraghty, \{Robert J.\} and Bonnac, \{Laurent F.\}",

note = "Publisher Copyright: {\textcopyright} 2023 by the authors.",

year = "2023",

month = mar,

doi = "10.3390/molecules28062616",

language = "English (US)",

volume = "28",

journal = "Molecules",

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T1 - Enhanced Remdesivir Analogues to Target SARS-CoV-2

AU - Majima, Ryuichi

AU - Edwards, Tiffany C.

AU - Dreis, Christine D.

AU - Geraghty, Robert J.

AU - Bonnac, Laurent F.

PY - 2023/3

Y1 - 2023/3

N2 - 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.

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.

KW - C-nucleoside

KW - SARS-CoV-2

KW - antiviral

KW - phosphate prodrug

UR - https://www.scopus.com/pages/publications/85151108059

UR - https://www.scopus.com/pages/publications/85151108059#tab=citedBy

U2 - 10.3390/molecules28062616

DO - 10.3390/molecules28062616

M3 - Article

C2 - 36985586

AN - SCOPUS:85151108059

SN - 1420-3049

VL - 28

JO - Molecules

JF - Molecules

IS - 6

M1 - 2616

ER -

Enhanced Remdesivir Analogues to Target SARS-CoV-2

Abstract

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