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Editors

Guest Editor
Dr. Jean Jacques Vanden Eynde

Formerly head of the Department of Organic Chemistry (FS), University of Mons-UMONS, 7000 Mons, Belgium
Website | E-Mail
Interests: heterocycles; microwave-induced synthesis; medicinal chemistry; green chemistry
Guest Editor
Dr. Annie Mayence

Formerly professor at the Haute Ecole Provinciale de Hainaut-Condorcet, 7330 Saint-Ghislain, Belgium
Website | E-Mail
Interests: medicinal chemistry, organic synthesis, parasitic diseases, orphan drugs

Topical Collection Information

Dear Colleagues,

The attention of our Editorial Board Members and Guest Editors is often attracted to exciting works covering their research interests, promising fields involved in drug discovery and development, as well as other hot and favorite scientific topics. To express that enthusiasm, Editorial Board Members invited leading investigators and asked them to share their knowledge with the readers of our journal Pharmaceuticals. Articles and reviews gathered in this Special Issue, thus, have the ambition to provide updated information on recent and outstanding findings. We hope that you will enjoy reading them.

Dr. Jean Jacques Vanden Eynde
Dr. Annie Mayence
Guest Editors

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 collection 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. Pharmaceuticals is an international peer-reviewed open access quarterly 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 850 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.

Published Papers (14 papers)

2017

Jump to: 2016, 2015

Open AccessReview Essential Oils and Antifungal Activity
Pharmaceuticals 2017, 10(4), 86; doi:10.3390/ph10040086
Received: 13 October 2017 / Revised: 27 October 2017 / Accepted: 30 October 2017 / Published: 2 November 2017
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Abstract
Since ancient times, folk medicine and agro-food science have benefitted from the use of plant derivatives, such as essential oils, to combat different diseases, as well as to preserve food. In Nature, essential oils play a fundamental role in protecting the plant from
[...] Read more.
Since ancient times, folk medicine and agro-food science have benefitted from the use of plant derivatives, such as essential oils, to combat different diseases, as well as to preserve food. In Nature, essential oils play a fundamental role in protecting the plant from biotic and abiotic attacks to which it may be subjected. Many researchers have analyzed in detail the modes of action of essential oils and most of their components. The purpose of this brief review is to describe the properties of essential oils, principally as antifungal agents, and their role in blocking cell communication mechanisms, fungal biofilm formation, and mycotoxin production. Full article
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Open AccessFeature PaperArticle Synthesis of Nitric Oxide Donors Derived from Piloty’s Acid and Study of Their Effects on Dopamine Secretion from PC12 Cells
Pharmaceuticals 2017, 10(3), 74; doi:10.3390/ph10030074
Received: 11 June 2017 / Revised: 28 August 2017 / Accepted: 30 August 2017 / Published: 5 September 2017
PDF Full-text (3233 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
This study investigated the mechanisms and kinetics of nitric oxide (NO) generation by derivatives of Piloty’s acid (NO-donors) under physiological conditions. In order to qualitatively and quantitatively measure NO release, electron paramagnetic resonance (EPR) was carried out with NO spin trapping. In addition,
[...] Read more.
This study investigated the mechanisms and kinetics of nitric oxide (NO) generation by derivatives of Piloty’s acid (NO-donors) under physiological conditions. In order to qualitatively and quantitatively measure NO release, electron paramagnetic resonance (EPR) was carried out with NO spin trapping. In addition, voltammetric techniques, including cyclic voltammetry and constant potential amperometry, were used to confirm NO release from Piloty’s acid and its derivatives. The resulting data showed that Piloty’s acid derivatives are able to release NO under physiological conditions. In particular, electron-withdrawing substituents favoured NO generation, while electron-donor groups reduced NO generation. In vitro microdialysis, performed on PC12 cell cultures, was used to evaluate the dynamical secretion of dopamine induced by the Piloty’s acid derivatives. Although all the studied molecules were able to induce DA secretion from PC12, only those with a slow release of NO have not determined an autoxidation of DA itself. These results confirm that the time-course of NO-donors decomposition and the amount of NO released play a key role in dopamine secretion and auto-oxidation. This information could drive the synthesis or the selection of compounds to use as potential drugs for the therapy of Parkinson’s disease (PD). Full article
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Open AccessArticle Individual and Combined Effects of Engineered Peptides and Antibiotics on Pseudomonas aeruginosa Biofilms
Pharmaceuticals 2017, 10(3), 58; doi:10.3390/ph10030058
Received: 26 May 2017 / Revised: 22 June 2017 / Accepted: 23 June 2017 / Published: 25 June 2017
PDF Full-text (3436 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Pseudomonas aeruginosa is involved in a variety of difficult-to-treat infections frequently due to biofilm formation. To identify useful antibiofilm strategies, this article evaluated efficacy of two newly engineered cationic antimicrobial peptides (17BIPHE2 and DASamP2), traditional antibiotics, and their combinations against biofilms at different
[...] Read more.
Pseudomonas aeruginosa is involved in a variety of difficult-to-treat infections frequently due to biofilm formation. To identify useful antibiofilm strategies, this article evaluated efficacy of two newly engineered cationic antimicrobial peptides (17BIPHE2 and DASamP2), traditional antibiotics, and their combinations against biofilms at different stages. 17BIPHE2 is designed based on the 3D structure of human cathelicidin LL-37 and DASamP2 is derived from database screening. While both peptides show effects on bacterial adhesion, biofilm formation, and preformed biofilms, select antibiotics only inhibit biofilm formation, probably due to direct bacterial killing. In addition, the time dependence of biofilm formation and treatment in a static in vitro biofilm model was also studied. The initial bacterial inoculum determines the peptide concentration needed to inhibit biofilm growth. When the bacterial growth time is less than 8 h, the biomass in the wells can be dispersed by either antibiotics alone or peptides alone. However, nearly complete biofilm disruption can be achieved when both the peptide and antibiotics are applied. Our results emphasize the importance of antibiofilm peptides, early treatment using monotherapy, and the combination therapy for already formed biofilms of P. aeruginosa. Full article
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Open AccessArticle Barriers to the Access of Bevacizumab in Patients with Solid Tumors and the Potential Impact of Biosimilars: A Physician Survey
Pharmaceuticals 2017, 10(1), 19; doi:10.3390/ph10010019
Received: 2 December 2016 / Revised: 23 January 2017 / Accepted: 23 January 2017 / Published: 28 January 2017
Cited by 1 | PDF Full-text (762 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Access to bevacizumab, an important component of oncology treatment regimens, may be limited. This survey of oncologists in the US (n = 150), Europe (n = 230), and emerging markets (EM: Brazil, Mexico, and Turkey; n = 130) examined use of
[...] Read more.
Access to bevacizumab, an important component of oncology treatment regimens, may be limited. This survey of oncologists in the US (n = 150), Europe (n = 230), and emerging markets (EM: Brazil, Mexico, and Turkey; n = 130) examined use of and barriers to accessing bevacizumab as treatment of advanced solid tumors. We also assessed the likelihood that physicians would prescribe a bevacizumab biosimilar, if available. Bevacizumab was frequently used as early-line therapy in metastatic colorectal cancer, metastatic non-squamous non–small-cell lung cancer, and metastatic ovarian cancer (all markets), and as a second-line therapy in glioblastoma multiforme (US, EM). A greater percentage of EM-based physicians cited access-related issues as a barrier to prescribing bevacizumab versus US and EU physicians. Lack of reimbursement and high out-of-pocket costs were cited as predominant barriers to prescribing and common reasons for reducing the number of planned cycles. Overall, ~50% of physicians reported they “definitely” or “probably” would prescribe a bevacizumab biosimilar, if available. Efficacy and safety data in specific tumor types and lower cost were factors cited that would increase likelihood to prescribe a bevacizumab biosimilar. A lower cost bevacizumab biosimilar could address the unmet needs of patients and physicians worldwide, and may have the greatest impact on patient outcomes in EM. Full article
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Open AccessMeeting Report “The 24th Conference” of the Groupement des Pharmacochimistes de l’Arc Atlantique (GP2A)
Pharmaceuticals 2017, 10(1), 17; doi:10.3390/ph10010017
Received: 12 December 2016 / Revised: 17 January 2017 / Accepted: 17 January 2017 / Published: 28 January 2017
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Abstract
The GP2A European Conference is a two-day meeting focused on medicinal chemistry and the use of tools to explore all fields of drug discovery and drug design such as molecular modelling, bioorganic chemistry, MS studies, in vitro in vivo assays, and structure activity
[...] Read more.
The GP2A European Conference is a two-day meeting focused on medicinal chemistry and the use of tools to explore all fields of drug discovery and drug design such as molecular modelling, bioorganic chemistry, MS studies, in vitro in vivo assays, and structure activity relationships. Abstracts of keynote lectures, plenary lectures, junior lectures, flash presentations, and posters presented during the meeting are collated in this report. Full article

2016

Jump to: 2017, 2015

Open AccessMeeting Report 30ièmes Journées Franco-Belges de Pharmacochimie
Pharmaceuticals 2016, 9(4), 73; doi:10.3390/ph9040073
Received: 8 November 2016 / Accepted: 10 November 2016 / Published: 18 November 2016
PDF Full-text (5531 KB) | HTML Full-text | XML Full-text
Abstract
The “Journées Franco-Belges de Pharmacochimie” is a recognized annual meeting in organic and medicinal chemistry known for the quality of scientific exchange and conviviality. Young researchers were encouraged to present their work and share ideas with senior scientists. Abstracts of plenary lectures, oral
[...] Read more.
The “Journées Franco-Belges de Pharmacochimie” is a recognized annual meeting in organic and medicinal chemistry known for the quality of scientific exchange and conviviality. Young researchers were encouraged to present their work and share ideas with senior scientists. Abstracts of plenary lectures, oral communications, and posters presented during the meeting are collected in this report. Full article
Open AccessReview Tumor Heterogeneity, Single-Cell Sequencing, and Drug Resistance
Pharmaceuticals 2016, 9(2), 33; doi:10.3390/ph9020033
Received: 28 December 2015 / Revised: 13 June 2016 / Accepted: 14 June 2016 / Published: 16 June 2016
Cited by 9 | PDF Full-text (381 KB) | HTML Full-text | XML Full-text
Abstract
Tumor heterogeneity has been compared with Darwinian evolution and survival of the fittest. The evolutionary ecosystem of tumors consisting of heterogeneous tumor cell populations represents a considerable challenge to tumor therapy, since all genetically and phenotypically different subpopulations have to be efficiently killed
[...] Read more.
Tumor heterogeneity has been compared with Darwinian evolution and survival of the fittest. The evolutionary ecosystem of tumors consisting of heterogeneous tumor cell populations represents a considerable challenge to tumor therapy, since all genetically and phenotypically different subpopulations have to be efficiently killed by therapy. Otherwise, even small surviving subpopulations may cause repopulation and refractory tumors. Single-cell sequencing allows for a better understanding of the genomic principles of tumor heterogeneity and represents the basis for more successful tumor treatments. The isolation and sequencing of single tumor cells still represents a considerable technical challenge and consists of three major steps: (1) single cell isolation (e.g., by laser-capture microdissection), fluorescence-activated cell sorting, micromanipulation, whole genome amplification (e.g., with the help of Phi29 DNA polymerase), and transcriptome-wide next generation sequencing technologies (e.g., 454 pyrosequencing, Illumina sequencing, and other systems). Data demonstrating the feasibility of single-cell sequencing for monitoring the emergence of drug-resistant cell clones in patient samples are discussed herein. It is envisioned that single-cell sequencing will be a valuable asset to assist the design of regimens for personalized tumor therapies based on tumor subpopulation-specific genetic alterations in individual patients. Full article
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Open AccessReview How Efficient Is My (Medicinal) Chemistry?
Pharmaceuticals 2016, 9(2), 26; doi:10.3390/ph9020026
Received: 27 January 2016 / Revised: 3 May 2016 / Accepted: 10 May 2016 / Published: 16 May 2016
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Abstract
“Greening” a chemical transformation is not about only changing the nature of a solvent or decreasing the reaction temperature. There are metrics enabling a critical quantification of the efficiency of an experimental protocol. Some of them are applied to different sequences for the
[...] Read more.
“Greening” a chemical transformation is not about only changing the nature of a solvent or decreasing the reaction temperature. There are metrics enabling a critical quantification of the efficiency of an experimental protocol. Some of them are applied to different sequences for the preparation of paracetamol in order to understand their performance parameters and elucidate pathways for improvement. Full article
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Open AccessFeature PaperCommunication 3,1-Benzothiazines, 1,4-Benzodioxines and 1,4-Benzoxazines as Inhibitors of Matriptase-2: Outcome of a Focused Screening Approach
Pharmaceuticals 2016, 9(1), 2; doi:10.3390/ph9010002
Received: 27 October 2015 / Revised: 5 January 2016 / Accepted: 7 January 2016 / Published: 13 January 2016
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Abstract
The liver enzyme matriptase-2 is a multi-domain, transmembrane serine protease with an extracellular, C-terminal catalytic domain. Synthetic low-molecular weight inhibitors of matriptase-2 have potential as therapeutics to treat iron overload syndromes, in particular in patients with β-thalassemia. A sub-library of 64 compounds was
[...] Read more.
The liver enzyme matriptase-2 is a multi-domain, transmembrane serine protease with an extracellular, C-terminal catalytic domain. Synthetic low-molecular weight inhibitors of matriptase-2 have potential as therapeutics to treat iron overload syndromes, in particular in patients with β-thalassemia. A sub-library of 64 compounds was screened for matriptase-2 inhibition and several active compounds were identified. (S)-Ethyl 2-(benzyl(3-((4-carbamidoylphenoxy)methyl)-2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-2-oxoacetate ((S)-12) showed an IC50 value of less than 10 µM. Structure-activity relationships were discussed and proposals to design new matriptase-2 inhibitors were made. Full article
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2015

Jump to: 2017, 2016

Open AccessMeeting Report 1st Joint European Conference on Therapeutic Targets and Medicinal Chemistry (TTMC 2015)
Pharmaceuticals 2016, 9(1), 1; doi:10.3390/ph9010001
Received: 12 October 2015 / Revised: 18 November 2015 / Accepted: 20 November 2015 / Published: 26 December 2015
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Abstract
The European Conference on Therapeutic Targets and Medicinal Chemistry is a new two-day meeting on drug discovery that is focused on therapeutic targets and the use of tools to explore all fields of drug discovery and drug design such as molecular modelling, bioorganic
[...] Read more.
The European Conference on Therapeutic Targets and Medicinal Chemistry is a new two-day meeting on drug discovery that is focused on therapeutic targets and the use of tools to explore all fields of drug discovery and drug design such as molecular modelling, bioorganic chemistry, NMR studies, fragment screening, in vitro assays, in vivo assays, structure activity relationships, autodisplay. Abstracts of keynote lectures, plenary lectures, junior lectures, flash presentations, and posters presented during the meeting are collected in this report. Full article
Open AccessFeature PaperReview Hormesis: Decoding Two Sides of the Same Coin
Pharmaceuticals 2015, 8(4), 865-883; doi:10.3390/ph8040865
Received: 13 November 2015 / Revised: 9 December 2015 / Accepted: 11 December 2015 / Published: 16 December 2015
Cited by 5 | PDF Full-text (1063 KB) | HTML Full-text | XML Full-text
Abstract
In the paradigm of drug administration, determining the correct dosage of a therapeutic is often a challenge. Several drugs have been noted to demonstrate contradictory effects per se at high and low doses. This duality in function of a drug at different concentrations
[...] Read more.
In the paradigm of drug administration, determining the correct dosage of a therapeutic is often a challenge. Several drugs have been noted to demonstrate contradictory effects per se at high and low doses. This duality in function of a drug at different concentrations is known as hormesis. Therefore, it becomes necessary to study these biphasic functions in order to understand the mechanistic basis of their effects. In this article, we focus on different molecules and pathways associated with diseases that possess a duality in their function and thus prove to be the seat of hormesis. In particular, we have highlighted the pathways and factors involved in the progression of cancer and how the biphasic behavior of the molecules involved can alter the manifestations of cancer. Because of the pragmatic role that it exhibits, the imminent need is to draw attention to the concept of hormesis. Herein, we also discuss different stressors that trigger hormesis and how stress-mediated responses increase the overall adaptive response of an individual to stress stimulus. We talk about common pathways through which cancer progresses (such as nuclear factor erythroid 2-related factor 2-Kelch-like ECH-associated protein 1 (Nrf2-Keap1), sirtuin-forkhead box O (SIRT-FOXO) and others), analyzing how diverse molecules associated with these pathways conform to hormesis. Full article
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Open AccessMeeting Report 29ièmes Journées Franco-Belges de Pharmacochimie: Meeting Report
Pharmaceuticals 2015, 8(4), 758-777; doi:10.3390/ph8040758
Received: 19 June 2015 / Revised: 19 June 2015 / Accepted: 24 June 2015 / Published: 17 November 2015
PDF Full-text (726 KB) | HTML Full-text | XML Full-text
Abstract
The “Journées Franco-Belges de Pharmacochimie” is a recognized two-day annual meeting on Medicinal Chemistry that is renowned for the advanced science presented, conviviality, and outstanding opportunities for senior and young scientists to exchange knowledge. Abstracts of plenary lectures, oral communications, and posters presented
[...] Read more.
The “Journées Franco-Belges de Pharmacochimie” is a recognized two-day annual meeting on Medicinal Chemistry that is renowned for the advanced science presented, conviviality, and outstanding opportunities for senior and young scientists to exchange knowledge. Abstracts of plenary lectures, oral communications, and posters presented during the meeting are collected in this report. Full article
Open AccessConcept Paper Opioid Facilitation of β-Adrenergic Blockade: A New Pharmacological Condition?
Pharmaceuticals 2015, 8(4), 664-674; doi:10.3390/ph8040664
Received: 16 August 2015 / Revised: 15 September 2015 / Accepted: 17 September 2015 / Published: 25 September 2015
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Abstract
Recently, propranolol was suggested to prevent hyperlactatemia in a child with hypovolemic shock through β-adrenergic blockade. Though it is a known inhibitor of glycolysis, propranolol, outside this observation, has never been reported to fully protect against lactate overproduction. On the other hand, literature
[...] Read more.
Recently, propranolol was suggested to prevent hyperlactatemia in a child with hypovolemic shock through β-adrenergic blockade. Though it is a known inhibitor of glycolysis, propranolol, outside this observation, has never been reported to fully protect against lactate overproduction. On the other hand, literature evidence exists for a cross-talk between β-adrenergic receptors (protein targets of propranolol) and δ-opioid receptor. In this literature context, it is hypothesized here that anti-diarrheic racecadotril (a pro-drug of thiorphan, an inhibitor of enkephalinases), which, in the cited observation, was co-administered with propranolol, might have facilitated the β-blocker-driven inhibition of glycolysis and resulting lactate production. The opioid-facilitated β-adrenergic blockade would be essentially additivity or even synergism putatively existing between antagonism of β-adrenergic receptors and agonism of δ-opioid receptor in lowering cellular cAMP and dependent functions. Full article
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Open AccessReview Antimicrobial Peptides in 2014
Pharmaceuticals 2015, 8(1), 123-150; doi:10.3390/ph8010123
Received: 11 February 2015 / Revised: 16 March 2015 / Accepted: 17 March 2015 / Published: 23 March 2015
Cited by 47 | PDF Full-text (1113 KB) | HTML Full-text | XML Full-text
Abstract
This article highlights new members, novel mechanisms of action, new functions, and interesting applications of antimicrobial peptides reported in 2014. As of December 2014, over 100 new peptides were registered into the Antimicrobial Peptide Database, increasing the total number of entries to 2493.
[...] Read more.
This article highlights new members, novel mechanisms of action, new functions, and interesting applications of antimicrobial peptides reported in 2014. As of December 2014, over 100 new peptides were registered into the Antimicrobial Peptide Database, increasing the total number of entries to 2493. Unique antimicrobial peptides have been identified from marine bacteria, fungi, and plants. Environmental conditions clearly influence peptide activity or function. Human α-defensin HD-6 is only antimicrobial under reduced conditions. The pH-dependent oligomerization of human cathelicidin LL-37 is linked to double-stranded RNA delivery to endosomes, where the acidic pH triggers the dissociation of the peptide aggregate to release its cargo. Proline-rich peptides, previously known to bind to heat shock proteins, are shown to inhibit protein synthesis. A model antimicrobial peptide is demonstrated to have multiple hits on bacteria, including surface protein delocalization. While cell surface modification to decrease cationic peptide binding is a recognized resistance mechanism for pathogenic bacteria, it is also used as a survival strategy for commensal bacteria. The year 2014 also witnessed continued efforts in exploiting potential applications of antimicrobial peptides. We highlight 3D structure-based design of peptide antimicrobials and vaccines, surface coating, delivery systems, and microbial detection devices involving antimicrobial peptides. The 2014 results also support that combination therapy is preferred over monotherapy in treating biofilms. Full article
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