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Selected Papers from the 4th International Electronic Conference on Medicinal...
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Selected Papers from the 4th International Electronic Conference on Medicinal Chemistry

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (31 October 2019) | Viewed by 26174

Special Issue Editor

Dr. Jean Jacques Vanden Eynde

E-Mail Website1 Website2
Guest Editor
Formerly Head, Department of Organic Chemistry (FS), University of Mons-UMONS, 7000 Mons, Belgium
Interests: heterocycles; medicinal chemistry; green chemistry; microwave-induced synthesis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue comprises selected papers from the 4th International Electronic Conference on Medicinal Chemistry (ECMC-4), held 1–30 November 2018, on sciforum.net, an online platform for hosting scholarly e-conferences and discussion groups. For more information on ECMC-4, please go to: http://sciforum.net/conference/ecmc-4.

Dr. Jean Jacques Vanden Eynde
Guest Editor

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Published Papers (5 papers)

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Research

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58 pages, 10961 KiB  
Article
Design, Synthesis and Biochemical Evaluation of Novel Ethanoanthracenes and Related Compounds to Target Burkitt’s Lymphoma
by Andrew J. Byrne, Sandra A. Bright, James P. McKeown, John E. O’Brien, Brendan Twamley, Darren Fayne, D. Clive Williams and Mary J. Meegan
Pharmaceuticals 2020, 13(1), 16; https://doi.org/10.3390/ph13010016 - 17 Jan 2020
Cited by 7 | Viewed by 5514
Abstract
Lymphomas (cancers of the lymphatic system) account for 12% of malignant diseases worldwide. Burkitt’s lymphoma (BL) is a rare form of non-Hodgkin’s lymphoma in which the cancer starts in the immune B-cells. We report the synthesis and preliminary studies on the antiproliferative activity [...] Read more.
Lymphomas (cancers of the lymphatic system) account for 12% of malignant diseases worldwide. Burkitt’s lymphoma (BL) is a rare form of non-Hodgkin’s lymphoma in which the cancer starts in the immune B-cells. We report the synthesis and preliminary studies on the antiproliferative activity of a library of 9,10-dihydro-9,10-ethanoanthracene based compounds structurally related to the antidepressant drug maprotiline against BL cell lines MUTU-1 and DG-75. Structural modifications were achieved by Diels-Alder reaction of the core 9-(2-nitrovinyl)anthracene with number of dienophiles including maleic anhydride, maleimides, acrylonitrile and benzyne. The antiproliferative activity of these compounds was evaluated in BL cell lines EBV− MUTU-1 and EBV+ DG-75 (chemoresistant). The most potent compounds 13j, 15, 16a, 16b, 16c, 16d and 19a displayed IC50 values in the range 0.17–0.38 μM against the BL cell line EBV− MUTU-1 and IC50 values in the range 0.45–0.78 μM against the chemoresistant BL cell line EBV+ DG-75. Compounds 15, 16b and 16c demonstrated potent ROS dependent apoptotic effects on the BL cell lines which were superior to the control drug taxol and showed minimal cytotoxicity to peripheral blood mononuclear cells (PBMCs). The results suggest that this class of compounds merits further investigation as antiproliferative agents for BL. Full article
(This article belongs to the Special Issue Selected Papers from the 4th International Electronic Conference on Medicinal Chemistry)
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28 pages, 5311 KiB  
Article
Hydroxypyridinone-Diamine Hybrids as Potential Neuroprotective Agents in the PC12 Cell-Line Model of Alzheimer’s Disease
by Elodie Lohou, N. André Sasaki, Agnès Boullier, Marine Duplantier and Pascal Sonnet
Pharmaceuticals 2019, 12(4), 162; https://doi.org/10.3390/ph12040162 - 27 Oct 2019
Cited by 7 | Viewed by 4308
Abstract
There is an urgent need to propose effective treatments for Alzheimer’s disease (AD). Although the origin of the disease is poorly understood, several therapeutic options have been proposed. The new therapeutic approaches targeting biometal-mediated neurodegenerative pathways appear to be interesting ones. As a [...] Read more.
There is an urgent need to propose effective treatments for Alzheimer’s disease (AD). Although the origin of the disease is poorly understood, several therapeutic options have been proposed. The new therapeutic approaches targeting biometal-mediated neurodegenerative pathways appear to be interesting ones. As a continuation of our preceding studies, two novel series of advanced glycation endproducts (AGE)/advanced lipid peroxidation endproducts (ALE) inhibitors have been developed as multifunctional scavengers. This extended work allowed us to highlight the new hydroxypyridinone-diamine hybrid IIa-3 bearing a C4 alkyl linker between the two pharmacophores. This derivative exhibited preserved potent capacities to trap reactive carbonyl species (vicinal diamine function) as well as reactive oxygen species and transition metals (hydroxypyridinone moiety) in comparison with previously described lead compound 1. In addition, its good predicted absorption, distribution, metabolism and excretion (ADME) properties were correlated with a better efficacy to inhibit in vitro methylglyoxal-induced apoptosis in neuronal-like PC12 cells. This new promising agent revealed improved druglikeness and ability to prevent biometal-mediated oxidative and carbonyl stress amplification involved in AD pathogenesis. Full article
(This article belongs to the Special Issue Selected Papers from the 4th International Electronic Conference on Medicinal Chemistry)
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17 pages, 1732 KiB  
Article
Synthesis and Study of New Quinolineaminoethanols as Anti-Bacterial Drugs
by Pierre Laumaillé, Alexandra Dassonville-Klimpt, François Peltier, Catherine Mullié, Claire Andréjak, Sophie Da-Nascimento, Sandrine Castelain and Pascal Sonnet
Pharmaceuticals 2019, 12(2), 91; https://doi.org/10.3390/ph12020091 - 18 Jun 2019
Cited by 2 | Viewed by 4036
Abstract
The lack of antibiotics with a novel mode of action associated with the spread of drug resistant bacteria make the fight against infectious diseases particularly challenging. A quinoline core is found in several anti-infectious drugs, such as mefloquine and bedaquiline. Two main objectives [...] Read more.
The lack of antibiotics with a novel mode of action associated with the spread of drug resistant bacteria make the fight against infectious diseases particularly challenging. A quinoline core is found in several anti-infectious drugs, such as mefloquine and bedaquiline. Two main objectives were set in this work. Firstly, we evaluated the anti-mycobacterial properties of the previous quinolines 3, which have been identified as good candidates against ESKAPEE (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter spp. and Escherichia coli) bacteria. Secondly, a new series 4 was designed and assessed against the same bacteria strains, taking the pair of enantiomers 3m/3n as the lead. More than twenty compounds 4 were prepared through a five-step asymmetric synthesis with good enantiomeric excesses (>90%). Interestingly, all compounds of series 3 were efficient on M. avium with MIC = 2–16 µg/mL, while series 4 was less active. Both series 3 and 4 were generally more active than mefloquine against the ESKAPEE bacteria. The quinolines 4 were either active against Gram-positive bacteria (MIC ≤ 4 µg/mL for 4c–4h and 4k/4l) or E. coli (MIC = 32–64 µg/mL for 4q–4v) according to the global lipophilicity of these compounds. Full article
(This article belongs to the Special Issue Selected Papers from the 4th International Electronic Conference on Medicinal Chemistry)
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17 pages, 1909 KiB  
Article
De Novo Design and In Vitro Testing of Antimicrobial Peptides against Gram-Negative Bacteria
by Boris Vishnepolsky, George Zaalishvili, Margarita Karapetian, Tornike Nasrashvili, Nato Kuljanishvili, Andrei Gabrielian, Alex Rosenthal, Darrell E. Hurt, Michael Tartakovsky, Maya Grigolava and Malak Pirtskhalava
Pharmaceuticals 2019, 12(2), 82; https://doi.org/10.3390/ph12020082 - 3 Jun 2019
Cited by 47 | Viewed by 6995
Abstract
Antimicrobial peptides (AMPs) have been identified as a potentially new class of antibiotics to combat bacterial resistance to conventional drugs. The design of de novo AMPs with high therapeutic indexes, low cost of synthesis, high resistance to proteases and high bioavailability remains a [...] Read more.
Antimicrobial peptides (AMPs) have been identified as a potentially new class of antibiotics to combat bacterial resistance to conventional drugs. The design of de novo AMPs with high therapeutic indexes, low cost of synthesis, high resistance to proteases and high bioavailability remains a challenge. Such design requires computational modeling of antimicrobial properties. Currently, most computational methods cannot accurately calculate antimicrobial potency against particular strains of bacterial pathogens. We developed a tool for AMP prediction (Special Prediction (SP) tool) and made it available on our Web site (https://dbaasp.org/prediction). Based on this tool, a simple algorithm for the design of de novo AMPs (DSP) was created. We used DSP to design short peptides with high therapeutic indexes against gram-negative bacteria. The predicted peptides have been synthesized and tested in vitro against a panel of gram-negative bacteria, including drug resistant ones. Predicted activity against Escherichia coli ATCC 25922 was experimentally confirmed for 14 out of 15 peptides. Further improvements for designed peptides included the synthesis of D-enantiomers, which are traditionally used to increase resistance against proteases. One synthetic D-peptide (SP15D) possesses one of the lowest values of minimum inhibitory concentration (MIC) among all DBAASP database short peptides at the time of the submission of this article, while being highly stable against proteases and having a high therapeutic index. The mode of anti-bacterial action, assessed by fluorescence microscopy, shows that SP15D acts similarly to cell penetrating peptides. SP15D can be considered a promising candidate for the development of peptide antibiotics. We plan further exploratory studies with the SP tool, aiming at finding peptides which are active against other pathogenic organisms. Full article
(This article belongs to the Special Issue Selected Papers from the 4th International Electronic Conference on Medicinal Chemistry)
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Review

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14 pages, 3890 KiB  
Review
Potential of the Other Genetic Information Coded by the Viral RNA Genomes as Antiviral Target
by Alfredo Berzal-Herranz, Cristina Romero-López, Beatriz Berzal-Herranz and Sara Ramos-Lorente
Pharmaceuticals 2019, 12(1), 38; https://doi.org/10.3390/ph12010038 - 13 Mar 2019
Cited by 4 | Viewed by 4120
Abstract
In addition to the protein coding information, viral RNA genomes code functional information in structurally conserved units termed functional RNA domains. These RNA domains play essential roles in the viral cycle (e.g., replication and translation). Understanding the molecular mechanisms behind their function is [...] Read more.
In addition to the protein coding information, viral RNA genomes code functional information in structurally conserved units termed functional RNA domains. These RNA domains play essential roles in the viral cycle (e.g., replication and translation). Understanding the molecular mechanisms behind their function is essential to understanding the viral infective cycle. Further, interfering with the function of the genomic RNA domains offers a potential means of developing antiviral strategies. Aptamers are good candidates for targeting structural RNA domains. Besides its potential as therapeutics, aptamers also provide an excellent tool for investigating the functionality of RNA domains in viral genomes. This review briefly summarizes the work carried out in our laboratory aimed at the structural and functional characterization of the hepatitis C virus (HCV) genomic RNA domains. It also describes the efforts we carried out for the development of antiviral aptamers targeting specific genomic domains of the HCV and the human immunodeficiency virus type-1 (HIV-1). Full article
(This article belongs to the Special Issue Selected Papers from the 4th International Electronic Conference on Medicinal Chemistry)
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