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Nucleosides: Synthesis and Antiviral Activity

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (31 October 2019) | Viewed by 10570

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,

For the last few decades, viral infectious diseases have continued to be a major health concern worldwide, causing relevant epidemiological, financial, and logistical implications. The use of many conventional drugs is hampered by a lack of efficacy, 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 aggressive and potentially fatal diseases, also including cancer and bacterial infections, remain important challenges. Chemical literature in this field is constantly growing and reports extremely valuable synthetic strategies that apply old and new chemical reactions to prepare a wide variety of nucleosides and analogs in high yields in few synthetic steps and with remarkably lower costs.

This Special Issue aims to attract contributions on all the aspects concerning the synthesis, through various and different strategies, of classical nucleosides, carbocyclic nucleoside, and analogs. 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 exploring the range of biological effects and potential applications as antivirals of brand-new compounds.

Prof. Dr. Paolo Quadrelli
Guest Editor

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Keywords

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

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Published Papers (1 paper)

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Review

35 pages, 8156 KiB  
Review
Stapled Peptides—A Useful Improvement for Peptide-Based Drugs
by Mattia Moiola, Misal G. Memeo and Paolo Quadrelli
Molecules 2019, 24(20), 3654; https://doi.org/10.3390/molecules24203654 - 10 Oct 2019
Cited by 107 | Viewed by 10069
Abstract
Peptide-based drugs, despite being relegated as niche pharmaceuticals for years, are now capturing more and more attention from the scientific community. The main problem for these kinds of pharmacological compounds was the low degree of cellular uptake, which relegates the application of peptide-drugs [...] Read more.
Peptide-based drugs, despite being relegated as niche pharmaceuticals for years, are now capturing more and more attention from the scientific community. The main problem for these kinds of pharmacological compounds was the low degree of cellular uptake, which relegates the application of peptide-drugs to extracellular targets. In recent years, many new techniques have been developed in order to bypass the intrinsic problem of this kind of pharmaceuticals. One of these features is the use of stapled peptides. Stapled peptides consist of peptide chains that bring an external brace that force the peptide structure into an α -helical one. The cross-link is obtained by the linkage of the side chains of opportune-modified amino acids posed at the right distance inside the peptide chain. In this account, we report the main stapling methodologies currently employed or under development and the synthetic pathways involved in the amino acid modifications. Moreover, we report the results of two comparative studies upon different kinds of stapled-peptides, evaluating the properties given from each typology of staple to the target peptide and discussing the best choices for the use of this feature in peptide-drug synthesis. Full article
(This article belongs to the Special Issue Nucleosides: Synthesis and Antiviral Activity)
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