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  1. Article ; Online: RNA: The most attractive target in recent viral diseases.

    Rabie, Amgad M

    Chemical biology & drug design

    2023  Volume 103, Issue 1, Page(s) e14404

    Abstract: As an expert in the field of drug design and discovery, I tried, in this up-to-date perspective or commentary article, to recap and shed light on the previous and latest revolutionary strategies employed in medicinal and therapeutic chemistry to target ... ...

    Abstract As an expert in the field of drug design and discovery, I tried, in this up-to-date perspective or commentary article, to recap and shed light on the previous and latest revolutionary strategies employed in medicinal and therapeutic chemistry to target the principal viral weapon used by virulent RNA viruses (e.g., the severe acute respiratory syndrome coronavirus 2 "SARS-CoV-2") to infect humans and spread infections, the genomic RNA strands. These strategies act by taking advantage of the weakness points of this attractive bioweapon to disable or attack it (itself), accordingly stop the entire viral reproduction, and effectively end the severe microbial infections such as the coronavirus disease 2019 (COVID-19). The generation of respective slightly falsely-weaved RNA strands, either endogenously or exogenously, is the principal key for designing most of these therapeutic approaches.
    MeSH term(s) Humans ; RNA ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; RNA-Dependent RNA Polymerase ; SARS-CoV-2 ; COVID-19 ; RNA, Viral
    Chemical Substances RNA (63231-63-0) ; Antiviral Agents ; RNA-Dependent RNA Polymerase (EC 2.7.7.48) ; RNA, Viral
    Language English
    Publishing date 2023-12-13
    Publishing country England
    Document type Journal Article
    ZDB-ID 2216600-2
    ISSN 1747-0285 ; 1747-0277
    ISSN (online) 1747-0285
    ISSN 1747-0277
    DOI 10.1111/cbdd.14404
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Retraction Note: CoViTris2020 and ChloViD2020: a striking new hope in COVID-19 therapy.

    Rabie, Amgad M

    Molecular diversity

    2022  Volume 27, Issue 3, Page(s) 1529

    Language English
    Publishing date 2022-10-06
    Publishing country Netherlands
    Document type Retraction of Publication
    ZDB-ID 1376507-3
    ISSN 1573-501X ; 1381-1991
    ISSN (online) 1573-501X
    ISSN 1381-1991
    DOI 10.1007/s11030-022-10521-6
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  3. Article: Retraction Note to: Discovery of (

    Rabie, Amgad M

    Chemicke zvesti

    2022  Volume 76, Issue 9, Page(s) 5991

    Abstract: This retracts the article DOI: 10.1007/s11696-021-01640-9.]. ...

    Abstract [This retracts the article DOI: 10.1007/s11696-021-01640-9.].
    Language English
    Publishing date 2022-06-04
    Publishing country Germany
    Document type Retraction of Publication
    ZDB-ID 2252770-9
    ISSN 1336-9075 ; 0366-6352
    ISSN (online) 1336-9075
    ISSN 0366-6352
    DOI 10.1007/s11696-022-02315-9
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  4. Article: RETRACTED ARTICLE: Discovery of (

    Rabie, Amgad M

    publication RETRACTED

    Chemicke zvesti

    2021  Volume 75, Issue 9, Page(s) 4669–4685

    Language English
    Publishing date 2021-05-16
    Publishing country Germany
    Document type Journal Article ; Retracted Publication
    ZDB-ID 2252770-9
    ISSN 1336-9075 ; 0366-6352
    ISSN (online) 1336-9075
    ISSN 0366-6352
    DOI 10.1007/s11696-021-01640-9
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  5. Article ; Online: Potent Inhibitory Activities of the Adenosine Analogue Cordycepin on SARS-CoV-2 Replication.

    Rabie, Amgad M

    ACS omega

    2022  Volume 7, Issue 3, Page(s) 2960–2969

    Abstract: Nucleoside analogues are among the most successful bioactive classes of druglike compounds in pharmaceutical chemistry as they are well-known for their numerous effective bioactivities in humans, especially as antiviral and anticancer agents. Coronavirus ...

    Abstract Nucleoside analogues are among the most successful bioactive classes of druglike compounds in pharmaceutical chemistry as they are well-known for their numerous effective bioactivities in humans, especially as antiviral and anticancer agents. Coronavirus disease 2019 (COVID-19) is still untreatable, with its causing virus, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), continuing to wreak havoc on the ground everywhere. This complicated international situation urged all concerned scientists, including medicinal chemists and drug discoverers, to search for a potent anti-COVID-19 drug. Cordycepin (3'-deoxyadenosine) is a known natural adenosine analogue of fungal origin, which could also be synthetically produced. This bioactive phytochemical compound is characterized by several proven strong pharmacological actions that may effectively contribute to the comprehensive treatment of COVID-19, with the antiviral activities being the leading ones. Some new studies predicted the possible inhibitory affinities of cordycepin against the principal SARS-CoV-2 protein targets (
    Language English
    Publishing date 2022-01-11
    Publishing country United States
    Document type Journal Article
    ISSN 2470-1343
    ISSN (online) 2470-1343
    DOI 10.1021/acsomega.1c05998
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  6. Article ; Online: Efficacious Preclinical Repurposing of the Nucleoside Analogue Didanosine against COVID-19 Polymerase and Exonuclease.

    Rabie, Amgad M

    ACS omega

    2022  Volume 7, Issue 25, Page(s) 21385–21396

    Abstract: Analogues and derivatives of natural nucleosides/nucleotides are considered among the most successful bioactive species of drug-like compounds in modern medicinal chemistry, as they are well recognized for their diverse and efficient pharmacological ... ...

    Abstract Analogues and derivatives of natural nucleosides/nucleotides are considered among the most successful bioactive species of drug-like compounds in modern medicinal chemistry, as they are well recognized for their diverse and efficient pharmacological activities in humans, especially as antivirals and antitumors. Coronavirus disease 2019 (COVID-19) is still almost incurable, with its infectious viral microbe, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), continuing to wreak devastation around the world. This global crisis pushed all involved scientists, including drug discoverers and clinical researchers, to try to find an effective and broad-spectrum anti-COVID-19 drug. Didanosine (2',3'-dideoxyinosine, DDI) is a synthetic inosine/adenosine/guanosine analogue and highly active antiretroviral therapeutic agent used for the treatment of human immunodeficiency virus infection and acquired immunodeficiency syndrome (HIV/AIDS). This potent reverse-transcriptase inhibitor is characterized by proven strong pharmacological effects against the viral genome, which may successfully take part in the effective treatment of SARS-CoV-2/COVID-19. Additionally, targeting the pivotal SARS-CoV-2 replication enzyme, RNA-dependent RNA polymerase (RdRp), is a very successful tactic to combat COVID-19 irrespective of the SARS-CoV-2 variant type because RdRps are broadly conserved among all SARS-CoV-2 strains. Herein, the current study proved for the first time, using the
    Language English
    Publishing date 2022-06-13
    Publishing country United States
    Document type Journal Article
    ISSN 2470-1343
    ISSN (online) 2470-1343
    DOI 10.1021/acsomega.1c07095
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  7. Article ; Online: Potent Inhibitory Activities of the Adenosine Analogue Cordycepin on SARS-CoV‑2 Replication

    Amgad M. Rabie

    ACS Omega, Vol 7, Iss 3, Pp 2960-

    2022  Volume 2969

    Keywords Chemistry ; QD1-999
    Language English
    Publishing date 2022-01-01T00:00:00Z
    Publisher American Chemical Society
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  8. Article: Discovery of Taroxaz-104: The first potent antidote of SARS-CoV-2 VOC-202012/01 strain.

    Rabie, Amgad M

    Journal of molecular structure

    2021  Volume 1246, Page(s) 131106

    Abstract: Polyhydroxyphenols and nitrogenous heterocyclics are two of the most powerful active species of molecules in pharmaceutical chemistry, as each of them is renowned for its various bioactivities for humans. One of their outstanding actions is the antiviral ...

    Abstract Polyhydroxyphenols and nitrogenous heterocyclics are two of the most powerful active species of molecules in pharmaceutical chemistry, as each of them is renowned for its various bioactivities for humans. One of their outstanding actions is the antiviral activities, which clearly appear if the principal functional entities of both classes meet into one compound. The recent COVID-19 pandemic pushed us to computationally sift and assess our small library of synthetic 2-(3,4,5-trihydroxyphenyl)-1,3,4-oxadiazoles against the main coronaviral protein/enzymatic targets. Surprisingly, few ligands exhibited interesting low binding energies (strong inhibitory affinities) with some SARS-CoV-2 proteins, mainly the pivotal enzyme RNA-dependent RNA polymerase (nCoV-RdRp). One of these compounds was Taroxaz-104 (5,5'-{5,5'-[(1
    Language English
    Publishing date 2021-07-16
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 194476-9
    ISSN 0022-2860 ; 0377-046X
    ISSN 0022-2860 ; 0377-046X
    DOI 10.1016/j.molstruc.2021.131106
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    Zs.A 1205: Show issues Location:
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  9. Article ; Online: CoViTris2020 and ChloViD2020: a striking new hope in COVID-19 therapy.

    Rabie, Amgad M

    publication RETRACTED

    Molecular diversity

    2021  Volume 25, Issue 3, Page(s) 1839–1854

    Abstract: Designing anticoronavirus disease 2019 (anti-COVID-19) agents is the primary concern of medicinal chemists/drug designers nowadays. Repurposing of known active compounds against the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a new ... ...

    Abstract Designing anticoronavirus disease 2019 (anti-COVID-19) agents is the primary concern of medicinal chemists/drug designers nowadays. Repurposing of known active compounds against the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a new effective and time-saving trend in anti-COVID-19 drug discovery. Thorough inhibition of the coronaviral-2 proteins (i.e., multitarget inhibition) is a possible powerful favorable strategy for developing effectively potent drugs for COVID-19. In this new research study, I succeeded to repurpose the two antioxidant polyhydroxy-1,3,4-oxadiazole compounds CoViTris2020 and ChloViD2020 as the first multitarget coronaviral protein blockers with extremely higher potencies (reach about 65 and 304 times, for CoViTris2020, and 20 and 93 times, for ChloViD2020, more potent than remdesivir and favipiravir, respectively). These two 2,5-disubstituted-1,3,4-oxadiazoles were computationally studied (through molecular docking in almost all SARS-CoV-2 proteins) and biologically assessed (through a newly established robust in vitro anti-COVID-19 assay) for their anticoronaviral-2 bioactivities. The data obtained from the docking investigation showed that both ligands promisingly exhibited very strong inhibitory binding affinities with almost all docked enzymes (e.g., they displayed extremely lower binding energies of - 12.00 and - 9.60 kcal/mol, respectively, with the SARS-CoV-2 RNA-dependent RNA polymerase "RdRp"). The results of the biological assay revealed that CoViTris2020 and ChloViD2020 significantly displayed very high anti-COVID-19 activities (anti-SARS-CoV-2 EC
    MeSH term(s) Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; COVID-19/drug therapy ; Drug Repositioning ; Oxadiazoles/chemistry ; Oxadiazoles/pharmacology ; Oxadiazoles/therapeutic use
    Chemical Substances Antiviral Agents ; Oxadiazoles
    Language English
    Publishing date 2021-01-03
    Publishing country Netherlands
    Document type Journal Article ; Retracted Publication
    ZDB-ID 1376507-3
    ISSN 1573-501X ; 1381-1991
    ISSN (online) 1573-501X
    ISSN 1381-1991
    DOI 10.1007/s11030-020-10169-0
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    Zs.A 4946: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (2.OG)
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  10. Article ; Online: Cyanorona-20: The first potent anti-SARS-CoV-2 agent.

    Rabie, Amgad M

    International immunopharmacology

    2021  Volume 98, Page(s) 107831

    Abstract: Explicit hindrance and blockade of the viral RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 is considered one of the most promising and efficient approaches for developing highly potent remedies for COVID-19. However, almost all of the reported viral ... ...

    Abstract Explicit hindrance and blockade of the viral RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 is considered one of the most promising and efficient approaches for developing highly potent remedies for COVID-19. However, almost all of the reported viral RdRp inhibitors (either repurposed or new antiviral drugs) lack specific selectivity against the novel coronaviral RdRp and still at a beginning phase of advancement. Herein, I discovered and introduce a new pyrazine derivative, (E)-N-(4-cyanobenzylidene)-6-fluoro-3-hydroxypyrazine-2-carboxamide (cyanorona-20), as the first potent SARS-CoV-2 RdRp inhibitor with very high selectivity (209- and 45-fold more potent than favipiravir and remdesivir, respectively). This promising selective specific anti-COVID-19 compound is also deemed to be the first distinctive derivative of favipiravir. Cyanorona-20, the unprecedented nucleoside/nucleotide analog, was designed, synthesized, characterized, computationally studied, and biologically evaluated for its anti-COVID-19 actions (through a precise in vitro anti-COVID-19 assay). The results of the biological assay displayed that cyanorona-20 surprisingly exhibited very high and largely significant anti-COVID-19 activities (anti-SARS-CoV-2 EC
    MeSH term(s) Antiviral Agents/chemical synthesis ; Antiviral Agents/pharmacology ; COVID-19/diagnosis ; COVID-19/drug therapy ; COVID-19/virology ; Computer-Aided Design ; Drug Design ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/pharmacology ; Host-Pathogen Interactions ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Molecular Targeted Therapy ; RNA-Dependent RNA Polymerase/antagonists & inhibitors ; RNA-Dependent RNA Polymerase/metabolism ; SARS-CoV-2/drug effects ; SARS-CoV-2/enzymology ; SARS-CoV-2/growth & development ; Structure-Activity Relationship ; Virus Replication/drug effects
    Chemical Substances Antiviral Agents ; Enzyme Inhibitors ; RNA-Dependent RNA Polymerase (EC 2.7.7.48)
    Language English
    Publishing date 2021-05-29
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 2043785-7
    ISSN 1878-1705 ; 1567-5769
    ISSN (online) 1878-1705
    ISSN 1567-5769
    DOI 10.1016/j.intimp.2021.107831
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    Zs.A 5408: Show issues Location:
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