E-Mail Alert

Add your e-mail address to receive forthcoming issues of this journal:

Journal Browser

Journal Browser

Special Issue "Bioactive Nucleosides and Nucleotides"

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

Deadline for manuscript submissions: 31 October 2018

Special Issue Editor

Guest Editor
Prof. Dr. Christian Ducho

Department of Pharmacy, Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2 3, 66 123 Saarbrücken, Germany
Website | E-Mail
Interests: medicinal chemistry; antibiotics; natural products; nucleosides; oligonucleotides

Special Issue Information

Dear Colleagues,

It is my pleasure to announce this Special Issue of Molecules on "Bioactive Nucleosides and Nucleotides". Analogues of nucleosides and nucleotides have had a tremendous impact, not only as (bio)chemical tools, but particularly also as drugs for human therapy. Nucleoside and nucleotide derivatives are currently widely used to treat cancer and viral infections, with the introduction of the highly potent anti-HCV drug Sofosbuvir (a nucleotide prodrug) representing the most recent milestone. However, nucleosides also find increasing interest as antibacterial drug candidates, which are urgently needed in the context of emerging resistances against established antibiotics.

For this Special Issue, we welcome contributions from all fields of nucleoside and nucleotide chemistry, may they be related to fundamental science or potential pharmaceutical applications. This also includes work that is mainly or even exclusively focused on organic synthesis. The synthetic preparation of nucleoside and nucleotide analogues is not trivial, and I strongly feel that there is an unfortunate tendency to overlook this highly important part of our daily work as chemists.

Prof. Dr. Christian Ducho
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • nucleosides and nucleotides
  • organic synthesis
  • anti-cancer agents
  • antiviral agents
  • antibacterial agents
  • chemical tools and probes

Published Papers (2 papers)

View options order results:
result details:
Displaying articles 1-2
Export citation of selected articles as:

Research

Open AccessArticle Anti-Hepatitis C Virus Activity of Uridine Derivatives of 2-Deoxy Sugars
Molecules 2018, 23(7), 1547; https://doi.org/10.3390/molecules23071547
Received: 24 May 2018 / Revised: 22 June 2018 / Accepted: 26 June 2018 / Published: 27 June 2018
PDF Full-text (3251 KB) | HTML Full-text | XML Full-text
Abstract
Hepatitis C virus (HCV), the etiological agent of the most common and dangerous diseases of the liver, is a major health problem worldwide. Despite many attempts, there is still no vaccine available. Although many drugs have been approved for use mostly in combination
[...] Read more.
Hepatitis C virus (HCV), the etiological agent of the most common and dangerous diseases of the liver, is a major health problem worldwide. Despite many attempts, there is still no vaccine available. Although many drugs have been approved for use mostly in combination regimen, their high costs make them out of reach in less developed regions. Previously, we have synthesized a series of compounds belonging to uridine derivatives of 2-deoxy sugars and have proved that some of them possess antiviral activity against influenza A virus associated with N-glycosylation inhibition. Here, we analyze the antiviral properties of these compounds against HCV. Using cell culture-derived HCV (HCVcc), HCV pseudoparticles (HCVpp), and replicon cell lines, we have shown high anti-HCV activity of two compounds. Our results indicated that compounds 2 and 4 significantly reduced HCVcc propagation with IC50 values in low μM range. Further experiments using the HCVpp system confirmed that both compounds significantly impaired the infectivity of produced HCVpp due to the inhibition of the correct maturation of viral glycoproteins. Overall, our results suggest that inhibiting the glycosylation process might be a good target for new therapeutics not only against HCV, but other important viral pathogens which contain envelopes with highly glycosylated proteins. Full article
(This article belongs to the Special Issue Bioactive Nucleosides and Nucleotides)
Figures

Graphical abstract

Open AccessArticle Phosphorus Pentachloride Promoted gem-Dichlorination of 2′- and 3′-Deoxynucleosides
Molecules 2018, 23(6), 1457; https://doi.org/10.3390/molecules23061457
Received: 29 May 2018 / Revised: 11 June 2018 / Accepted: 11 June 2018 / Published: 15 June 2018
PDF Full-text (1561 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Halogen substitution at various positions of canonical nucleosides has generated a number of bioactive structural variants. Herein, the synthesis of two unique series of sugar modified nucleosides bearing a gem-dichloro group is presented. The synthetic plan entails the controlled addition of phosphorus
[...] Read more.
Halogen substitution at various positions of canonical nucleosides has generated a number of bioactive structural variants. Herein, the synthesis of two unique series of sugar modified nucleosides bearing a gem-dichloro group is presented. The synthetic plan entails the controlled addition of phosphorus pentachloride to suitably protected 2′- or 3′-ketodeoxynucleoside intermediates as the key step, facilitating the rapid construction of such functionalized molecules. Under the same reaction conditions, the highest chemoselectivity was observed for the formation of 2′,2′-dichloro-2′,3′-dideoxynucleosides, while a competing 2′,3′-elimination process occurred in the case of the 3′,3′-dichloro counterparts. Full article
(This article belongs to the Special Issue Bioactive Nucleosides and Nucleotides)
Figures

Graphical abstract

Back to Top