Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20)

Rabie, Amgad M.

Amgad M. Rabie

Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20)

Abstract:

Medicinal chemistry scientists' efforts and trials to discover a very potent anticoronaviral medicine specifically effective against the current frightening virus, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), are not over yet. Synthetic organic chemistry will remain one of the most important branches in the entire drug discovery science. (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20), a newly-discovered favipiravir analog/ derivative, is one of the promising synthetic organic compounds that displayed very strong nanomolar potencies against this fatal coronavirus, reaching an anticoronaviral-2 EC50 of nearly 450 nM or 0.45 μM. This compound was found to act against the SARS-CoV-2 mainly through the powerful inhibition of the coronaviral RNA-dependent RNA polymerase (RdRp), via competitively occupying and locking this enzyme's major catalytic active site pocket (the suggested primary mechanism of action). Cyanorona-20 is still under progressive investigation as an attempt to continue developing it as a prospective remedy for the coronavirus disease 2019 (COVID-19). However, the previous literature synthetic procedures of Cyanorona-20 were criticized for several reasons like the harsh handling, difficult separation, small yield, and low purity. Herein in this short-communication or technical-note article, more reproducible and efficient novel synthetic method for Cyanorona-20 compound is presented, in an effort to address almost all of the problems which were accompanying the preceding methods.

Keywords:
Anti-COVID-19 Medicine; SARS-CoV-2; Coronaviral-2 RNA-dependent RNA Polymerase (RdRp); Favipiravir; Drug Discovery; Cyanorona-20; Novel Synthesis; Optimized Synthetic Procedure; Monkeypox Virus (MPV) Inhibitor

Issue: 2022, Volume 73, Issue 4

Pages: 69-75

Publication date: 2022/10/31

https://doi.org/10.37358/RC.22.4.8555

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Citation Styles

Cite this article as:
RABIE, A.M., Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20), Rev. Chim., 73(4), 2022, 69-75.

Vancouver
Rabie AM. Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20). Rev. Chim.[internet]. 2022 Apr;73(4):69-75. Available from: https://doi.org/10.37358/RC.22.4.8555

APA 6th edition
Rabie, A.M., (2022). Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20). Revista de Chimie, 73(4), 69-75. https://doi.org/10.37358/RC.22.4.8555

Harvard
Rabie, A.M., (2022). 'Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20)', Revista de Chimie, 73(4), pp. 69-75. https://doi.org/10.37358/RC.22.4.8555

IEEE
A.M. Rabie, "Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20)". Revista de Chimie, vol. 73, no. 4, pp. 69-75, 2022. [online]. https://doi.org/10.37358/RC.22.4.8555

Text
Amgad M. Rabie,
Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20),
Revista de Chimie,
Volume 73, Issue 4,
2022,
Pages 69-75,
ISSN 2668-8212,
https://doi.org/10.37358/RC.22.4.8555.
(https://revistadechimie.ro/Articles.asp?ID=8555)
Keywords: Anti-COVID-19 Medicine; SARS-CoV-2; Coronaviral-2 RNA-dependent RNA Polymerase (RdRp); Favipiravir; Drug Discovery; Cyanorona-20; Novel Synthesis; Optimized Synthetic Procedure; Monkeypox Virus (MPV) Inhibitor

RIS
TY - JOUR
T1 - Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20)
A1 - Rabie, Amgad M.
JF - Revista de Chimie
JO - Rev. Chim.
PB - Revista de Chimie SRL
SN - 2668-8212
Y1 - 2022
VL - 73
IS - 4
SP - 69
EP - 75
UR - https://doi.org/10.37358/RC.22.4.8555
KW - Anti-COVID-19 Medicine
KW - SARS-CoV-2
KW - Coronaviral-2 RNA-dependent RNA Polymerase (RdRp)
KW - Favipiravir
KW - Drug Discovery
KW - Cyanorona-20
KW - Novel Synthesis
KW - Optimized Synthetic Procedure
KW - Monkeypox Virus (MPV) Inhibitor
ER -

BibTex
@article{RevCh2022P69,
author = {Rabie Amgad M.},
title = {Improved Synthesis of the Anti-SARS-CoV-2 Investigational Agent (E)-N-(4-Cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (Cyanorona-20)},
journal = {Revista de Chimie},
volume = {73},
number = {4},
pages = {69-75},
year = {2022},
issn = {2668-8212},
doi = {https://doi.org/10.37358/RC.22.4.8555},
url = {https://revistadechimie.ro/Articles.asp?ID=8555}
}

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