Your browser doesn't support javascript.
RETRACTED ARTICLE: Discovery of (E)-N-(4-cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (cyanorona-20): the first potent and specific anti-COVID-19 drug.
Rabie, Amgad M.
  • Rabie AM; Dr. Amgad Rabie's Research Lab. for Drug Discovery (DARLD), Mansoura, Egypt.
Chem Zvesti ; 75(9): 4669-4685, 2021.
Article in English | MEDLINE | ID: covidwho-1237549
Semantic information from SemMedBD (by NLM)
1. Pharmaceutical Preparations TREATS COVID-19
Subject
Pharmaceutical Preparations
Predicate
TREATS
Object
COVID-19
2. Inhibitor PART_OF 2019 novel coronavirus
Subject
Inhibitor
Predicate
PART_OF
Object
2019 novel coronavirus
3. Inhibitor compared_with favipiravir
Subject
Inhibitor
Predicate
compared_with
Object
favipiravir
4. Inhibitor higher_than favipiravir
Subject
Inhibitor
Predicate
higher_than
Object
favipiravir
5. Pharmaceutical Preparations DISRUPTS RNA-directed RNA polymerase activity
Subject
Pharmaceutical Preparations
Predicate
DISRUPTS
Object
RNA-directed RNA polymerase activity
6. favipiravir TREATS COVID-19
Subject
favipiravir
Predicate
TREATS
Object
COVID-19
7. Pharmaceutical Preparations TREATS COVID-19
Subject
Pharmaceutical Preparations
Predicate
TREATS
Object
COVID-19
8. Inhibitor PART_OF 2019 novel coronavirus
Subject
Inhibitor
Predicate
PART_OF
Object
2019 novel coronavirus
9. Inhibitor compared_with favipiravir
Subject
Inhibitor
Predicate
compared_with
Object
favipiravir
10. Inhibitor higher_than favipiravir
Subject
Inhibitor
Predicate
higher_than
Object
favipiravir
11. Pharmaceutical Preparations DISRUPTS RNA-directed RNA polymerase activity
Subject
Pharmaceutical Preparations
Predicate
DISRUPTS
Object
RNA-directed RNA polymerase activity
12. favipiravir TREATS COVID-19
Subject
favipiravir
Predicate
TREATS
Object
COVID-19
ABSTRACT
Abstract Specific inhibition of the viral RNA-dependent RNA polymerase (RdRp) of the newly-emerged severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a very promising strategy for developing highly potent medicines for coronavirus disease 2019 (COVID-19). However, almost all of the reported viral RdRp inhibitors (either repurposed drugs or new antiviral agents) lack selectivity against the SARS-CoV-2 RdRp. Herein, I discovered a new favipiravir derivative, (E)-N-(4-cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (cyanorona-20), as the first potent SARS-CoV-2 inhibitor with very high selectivity (209- and 45-fold more potent than favipiravir and remdesivir, respectively). Based on the significant reduction in the in vitro SARS-CoV-2 replication/copies, strong computational cyanorona-20 ligand-RdRp protein interactions, and anti-RdRp activity of the parent favipiravir drug, SARS-CoV-2 inhibition is thought to be mediated through the coronaviral-2 RdRp inhibition. This promising selective anti-COVID-19 compound is also, to the best of our knowledge, the first bioactive derivative of favipiravir, the known antiinfluenza and antiviral drug. This new nucleoside analog was designed, synthesized, characterized, computationally studied (through pharmacokinetic calculations along with computational molecular modeling and prediction), and biologically evaluated for its anti-COVID-19 activities (through a validated in vitro anti-COVID-19 assay). The results of the biological assay showed that cyanorona-20 surprisingly exhibited very significant anti-COVID-19 activity (anti-SARS-CoV-2 EC50 = 0.45 µM), and, in addition, it could be also a very promising lead compound for the design of new anti-COVID-19 agents. Cyanorona-20 is a new favipiravir derivative with promise for the treatment of SARS-CoV-2 infection. Supplementary Information The online version contains supplementary material available at 10.1007/s11696-021-01640-9.
Keywords

Full text: Available Collection: International databases Database: MEDLINE Type of study: Prognostic study Language: English Journal: Chem Zvesti Year: 2021 Document Type: Article Affiliation country: S11696-021-01640-9

Similar

MEDLINE

...
LILACS

LIS


Full text: Available Collection: International databases Database: MEDLINE Type of study: Prognostic study Language: English Journal: Chem Zvesti Year: 2021 Document Type: Article Affiliation country: S11696-021-01640-9