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Special Issue "Recent Advances in the Development of Antiviral Agents"

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

Deadline for manuscript submissions: 31 January 2019

Special Issue Editor

Guest Editor
Prof. Dr. Stefano Aquaro

Department of Pharmacy, Health and Nutritional Sciences Università della Calabria, Rende (CS), Italy
Website | E-Mail
Interests: virus evolution; macrophages; HIV pathogenesis; antivirals; HIV chemotherapy; neuroAIDS; mechanisms of virus entry; chemokines and chemokine receptors; role of astrocytes and neurones in HIV infection

Special Issue Information

Dear Colleagues, 

Viral infections inflict many serious human diseases, especially in the most developing countries, with very high mortality rates. New drug-resistant strains are continually emerging due to the high viral mutation rate, which makes it necessary to develop novel and possibly more potent antiviral compounds. All researchers working in this field are cordially invited to contribute original research papers or reviews to this Special Issue of Molecules, which will report on the design, synthesis, and evaluation of novel antiviral drug or microbicide candidates against viral infections, the identification of novel biological targets or therapeutic approaches and rationale, or studies about antiviral resistance mechanisms and strategies to prevent and/or circumvent them.

Prof. Dr. Stefano Aquaro
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

  • Antivirials
  • Drug design
  • Drug synthesis
  • Antiviral activity
  • Viruses
  • Antiviral resistence
  • Virus evolution
  • Antiviral therapy
  • Virus entry
  • Virus replication
  • Viral enzimes
  • Virus phatogenesis

Published Papers (3 papers)

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Research

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Open AccessArticle Synthesis and Evolution of Berberine Derivatives as a New Class of Antiviral Agents against Enterovirus 71 through the MEK/ERK Pathway and Autophagy
Molecules 2018, 23(8), 2084; https://doi.org/10.3390/molecules23082084
Received: 17 July 2018 / Revised: 14 August 2018 / Accepted: 16 August 2018 / Published: 20 August 2018
PDF Full-text (8860 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Taking berberine (BBR) as the lead, 23 new BBR derivatives were synthesized and examined for their antiviral activities against four different genotype enterovirus 71 (EV71) strains with a cytopathic effect (CPE) assay. Structure-activity relationship (SAR) studies indicated that introduction of a suitable substituent
[...] Read more.
Taking berberine (BBR) as the lead, 23 new BBR derivatives were synthesized and examined for their antiviral activities against four different genotype enterovirus 71 (EV71) strains with a cytopathic effect (CPE) assay. Structure-activity relationship (SAR) studies indicated that introduction of a suitable substituent at the 9-position might be beneficial for potency. Among them, compound 2d exhibited most potent activities with IC50 values of 7.12–14.8 μM, similar to that of BBR. The effect of 2d was further confirmed in a dose-dependent manner both in RNA and protein level. The mechanism revealed that 2d could inhibit the activation of MEK/ERK signaling pathway. Meanwhile, it could suppress the EV71-induced autophagy by activating AKT and inhibiting the phosphorylation of JNK and PI3KIII proteins. We consider BBR derivatives to be a new family of anti-EV71 agents through targeting host components, with an advantage of broad-spectrum anti-EV71 potency. Full article
(This article belongs to the Special Issue Recent Advances in the Development of Antiviral Agents)
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Open AccessArticle HIV-1 Integrase-Targeted Short Peptides Derived from a Viral Protein R Sequence
Molecules 2018, 23(8), 1858; https://doi.org/10.3390/molecules23081858
Received: 25 June 2018 / Revised: 18 July 2018 / Accepted: 23 July 2018 / Published: 26 July 2018
PDF Full-text (1992 KB) | HTML Full-text | XML Full-text
Abstract
HIV-1 integrase (IN) inhibitors represent a new class of highly effective anti-AIDS therapeutics. Current FDA-approved IN strand transfer inhibitors (INSTIs) share a common mechanism of action that involves chelation of catalytic divalent metal ions. However, the emergence of IN mutants having reduced sensitivity
[...] Read more.
HIV-1 integrase (IN) inhibitors represent a new class of highly effective anti-AIDS therapeutics. Current FDA-approved IN strand transfer inhibitors (INSTIs) share a common mechanism of action that involves chelation of catalytic divalent metal ions. However, the emergence of IN mutants having reduced sensitivity to these inhibitors underlies efforts to derive agents that antagonize IN function by alternate mechanisms. Integrase along with the 96-residue multifunctional accessory protein, viral protein R (Vpr), are both components of the HIV-1 pre-integration complex (PIC). Coordinated interactions within the PIC are important for viral replication. Herein, we report a 7-mer peptide based on the shortened Vpr (69–75) sequence containing a biotin group and a photo-reactive benzoylphenylalanyl residue, and which exhibits low micromolar IN inhibitory potency. Photo-crosslinking experiments have indicated that the peptide directly binds IN. The peptide does not interfere with IN-DNA interactions or induce higher-order, aberrant IN multimerization, suggesting a mode of action for the peptide that is distinct from clinically used INSTIs and developmental allosteric IN inhibitors. This compact Vpr-derived peptide may serve as a valuable pharmacological tool to identify a potential new pharmacologic site. Full article
(This article belongs to the Special Issue Recent Advances in the Development of Antiviral Agents)
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Other

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Open AccessBrief Report Combining New Non-Nucleoside Reverse Transcriptase Inhibitors (RTIs) with AZT Results in Strong Synergism against Multi-RTI-Resistant HIV-1 Strains
Molecules 2018, 23(7), 1599; https://doi.org/10.3390/molecules23071599
Received: 24 May 2018 / Revised: 21 June 2018 / Accepted: 28 June 2018 / Published: 2 July 2018
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Abstract
Reverse transcriptase inhibitors (RTIs), including nucleoside RTIs (NRTIs) and non-nucleoside RTIs (NNRTIs), are critical antiretroviral drugs for the treatment of human immunodeficiency virus (HIV) infection. Emergence of multi-RTI resistance calls for the development of more potent therapeutics or regimens against RTI-resistant strains. Here,
[...] Read more.
Reverse transcriptase inhibitors (RTIs), including nucleoside RTIs (NRTIs) and non-nucleoside RTIs (NNRTIs), are critical antiretroviral drugs for the treatment of human immunodeficiency virus (HIV) infection. Emergence of multi-RTI resistance calls for the development of more potent therapeutics or regimens against RTI-resistant strains. Here, we demonstrated that combining azidothymidine (AZT) with a new NNRTIs under development, diarylpyridine (DAPA)-2e, diarylanilin (DAAN)-14h, or DAAN-15h, resulted in strong synergism against infection by divergent HIV-1 strains, including those resistant to NRTIs and NNRTIs, suggesting the potential for developing these novel NNRTIs as salvage therapy for HIV/acquired immune deficiency syndrome (AIDS) patients. Full article
(This article belongs to the Special Issue Recent Advances in the Development of Antiviral Agents)
Figures

Graphical abstract

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