Synthesis and anti-SARS-CoV-2 evaluation of lipid prodrugs of β-D-N4-hydroxycytidine (NHC) and a 3′-fluoro-substituted analogue of NHC

ZH Wen, MM Wang, LY Li, P Herdewijn, R Snoeck… - Bioorganic …, 2023 - Elsevier
Abstract β-DN 4-hydroxycytidine (NHC, EIDD-1931) is a nucleoside analogue that exhibits
broad spectrum antiviral activity against a variety of RNA viruses. Herein, we report the …

Synthesis and Antiviral Activity of Novel β-D-N4-Hydroxycytidine Ester Prodrugs as Potential Compounds for the Treatment of SARS-CoV-2 and Other Human …

ES Darnotuk, AE Siniavin, NS Shastina, SI Luyksaar… - Pharmaceuticals, 2023 - mdpi.com
The spread of COVID-19 infection continues due to the emergence of multiple transmissible
and immune-evasive variants of the SARS-CoV-2 virus. Although various vaccines have …

[HTML][HTML] Synthesis and biological evaluation of new β-D-N4-hydroxycytidine analogs against SARS-CoV-2, influenza viruses and DENV-2

YJ An, SM Choi, ER Choi, YE Nam, EW Seo… - Bioorganic & Medicinal …, 2023 - Elsevier
Drug repurposing approach was applied to find a potent antiviral agent against RNA viruses
such as SARS-CoV-2, influenza viruses and dengue virus with a concise strategy of small …

Rethinking remdesivir: synthesis, antiviral activity, and pharmacokinetics of oral lipid prodrugs

RT Schooley, AF Carlin, JR Beadle… - Antimicrobial agents …, 2021 - Am Soc Microbiol
ABSTRACT Remdesivir (RDV; GS-5734) is currently the only FDA-approved antiviral drug
for the treatment of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) …

[HTML][HTML] New conjugates based on N4-hydroxycytidine with more potent antiviral efficacy in vitro than EIDD-2801 against SARS-CoV-2 and other human …

AE Siniavin, VA Gushchin, SS Natal'ya, ES Darnotuk… - Antiviral Research, 2024 - Elsevier
The spread of COVID-19 continues due to genetic variation in SARS-CoV-2. Highly mutated
variants of SARS-CoV-2 have an increased transmissibility and immune evasion. Due to the …

Broad spectrum antiviral nucleosides—Our best hope for the future

KL Seley-Radtke, JE Thames, CD Waters III - Annual reports in medicinal …, 2021 - Elsevier
The current focus for many researchers has turned to the development of therapeutics that
have the potential for serving as broad-spectrum inhibitors that can target numerous viruses …

Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2

D Wei, T Hu, Y Zhang, W Zheng, H Xue, J Shen… - Bioorganic & Medicinal …, 2021 - Elsevier
The nucleoside metabolite of remdesivir, GS-441524 displays potent anti-SARS-CoV-2
efficacy, and is being evaluated in clinical as an oral antiviral therapeutic for COVID-19 …

Nucleoside analogs and nucleoside precursors as drugs in the fight against SARS-CoV-2 and other coronaviruses

N Borbone, G Piccialli, GN Roviello, G Oliviero - Molecules, 2021 - mdpi.com
Coronaviruses (CoVs) are positive-sense RNA enveloped viruses, members of the family
Coronaviridae, that cause infections in a broad range of mammals including humans …

Synthesis and antiviral activity of fatty acyl conjugates of remdesivir against severe acute respiratory syndrome coronavirus 2 and Ebola virus

NS El-Sayed, AS Jureka, MR Edwards, S Lohan… - European Journal of …, 2021 - Elsevier
We report here the synthesis, purification, and characterization of mono-and di-fatty acyl
conjugates of remdesivir (RDV) and their in vitro antiviral activity against SAR-CoV-2, an …

[HTML][HTML] Enhanced broad spectrum in vitro antiviral efficacy of 3-F-4-MeO-Bn, 3-CN, and 4-CN derivatives of lipid remdesivir nucleoside monophosphate prodrugs

RE McMillan, MK Lo, XQ Zhang, JR Beadle, N Valiaeva… - Antiviral research, 2023 - Elsevier
Broad spectrum oral antivirals are urgently needed for the early treatment of many RNA
viruses of clinical concern. We previously described the synthesis of 1-O-octadecyl-2-O …