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Synthesis of Antiviral Compounds

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 October 2021) | Viewed by 5200

Special Issue Editor


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Guest Editor
Department of Chemistry, Università degli Studi di Pavia, Pavia, Italy
Interests: pericyclic reactions; 1,3-dipolar cycloadditions; hetero diels-alder reactions; antivirals; catalysis; polymers
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Special Issue Information

Dear Colleagues,

Viral infectious diseases continue to be a major health concern worldwide, causing relevant epidemiological, financial, and logistical implications, as we are experimenting in these months. The use of many conventional drugs is hampered by a lack of efficacy, the emergence of resistance, adverse effects, and high costs. Thus, new strategies and therapeutic alternatives are constantly needed. Nucleosides are fundamental building blocks of biological systems that show a wide range of biological activities. Consequently, extensive modifications have been made to both the heterocyclic base and the sugar moiety in order to avoid the drawbacks shown by nucleosides or analogues in certain applications, mainly due to enzymatic degradations. The design and synthesis of molecules for the fight against new aggressive and fatal diseases remain important challenges.

This Special Issue in Molecules aims to attract contributions on all the aspects concerning the synthesis through different strategies of classical nucleosides, carbocyclic nucleosides, and analogues. These results can be considered fully consistent if in vitro biological evaluations of the synthetized compounds are also reported. This will be the challenge to further explore the range of biological effects and potential applications as antivirals of brand-new compounds.

Prof. Dr. Paolo Quadrelli
Guest Editor

Manuscript Submission Information

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Keywords

  • Nucleosides
  • Nucleoside analogues
  • Synthetic strategy
  • Antivirals
  • Biological evaluation
  • Structure activity relationship

Published Papers (2 papers)

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Research

15 pages, 3060 KiB  
Article
Synthesis of Potential Antiviral Agents for SARS-CoV-2 Using Molecular Hybridization Approach
by Kailey A. Wyman, Adel S. Girgis, Pragnakiran S. Surapaneni, Jade M. Moore, Noura M. Abo Shama, Sara H. Mahmoud, Ahmed Mostafa, Reham F. Barghash, Zou Juan, Radha D. Dobaria, Ahmad J. Almalki, Tarek S. Ibrahim and Siva S. Panda
Molecules 2022, 27(18), 5923; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27185923 - 12 Sep 2022
Cited by 8 | Viewed by 1851
Abstract
We synthesized a set of small molecules using a molecular hybridization approach with good yields. The antiviral properties of the synthesized conjugates against the SAR-CoV-2 virus were investigated and their cytotoxicity was also determined. Among all the synthesized conjugates, compound 9f showed potential [...] Read more.
We synthesized a set of small molecules using a molecular hybridization approach with good yields. The antiviral properties of the synthesized conjugates against the SAR-CoV-2 virus were investigated and their cytotoxicity was also determined. Among all the synthesized conjugates, compound 9f showed potential against SARS-CoV-2 and low cytotoxicity. The conjugates’ selectivity indexes (SIs) were determined to correlate the antiviral properties and cytotoxicity. The observed biological data were further validated using computational studies. Full article
(This article belongs to the Special Issue Synthesis of Antiviral Compounds)
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18 pages, 4090 KiB  
Article
Synthesis and Antiviral Evaluation of (1,4-Disubstituted-1,2,3-Triazol)-(E)-2-Methyl-but-2-Enyl Nucleoside Phosphonate Prodrugs
by Tuniyazi Abuduaini, Vincent Roy, Julien Marlet, Catherine Gaudy-Graffin, Denys Brand, Cécile Baronti, Franck Touret, Bruno Coutard, Tamara R. McBrayer, Raymond F. Schinazi and Luigi A. Agrofoglio
Molecules 2021, 26(5), 1493; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26051493 - 09 Mar 2021
Cited by 4 | Viewed by 2751
Abstract
A series of hitherto unknown (1,4-disubstituted-1,2,3-triazol)-(E)-2-methyl-but-2-enyl nucleosides phosphonate prodrugs bearing 4-substituted-1,2,3-triazoles were prepared in a straight approach through an olefin acyclic cross metathesis as the key synthetic step. All novel compounds were evaluated for their antiviral activities against HBV, HIV and [...] Read more.
A series of hitherto unknown (1,4-disubstituted-1,2,3-triazol)-(E)-2-methyl-but-2-enyl nucleosides phosphonate prodrugs bearing 4-substituted-1,2,3-triazoles were prepared in a straight approach through an olefin acyclic cross metathesis as the key synthetic step. All novel compounds were evaluated for their antiviral activities against HBV, HIV and SARS-CoV-2. Among these molecules, only compound 15j, a hexadecyloxypropyl (HDP)/(isopropyloxycarbonyl-oxymethyl)-ester (POC) prodrug, showed activity against HBV in Huh7 cell cultures with 62% inhibition at 10 μM, without significant cytotoxicity (IC50 = 66.4 μM in HepG2 cells, IC50 = 43.1 μM in HepG2 cells) at 10 μM. Full article
(This article belongs to the Special Issue Synthesis of Antiviral Compounds)
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