Selected Papers from the 8th International Electronic Conference on Medicinal Chemistry (ECMC2022)

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (1 November 2023) | Viewed by 8069

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Department of Molecular Biology, Instituto de Parasitología y Biomedicina López-Neyra (IPBLN-CSIC), PTS Granada, Av del Conocimiento 17, 18016 Granada, Spain
Interests: antiviral nucleic acids; therapeutic RNA; aptamers; RNA inhibitors; structure/function of RNA; RNA viruses
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1. Interdisciplinary Centre of Marine and Environmental Research (CIIMAR), 4450-208 Porto, Portugal
2. Laboratory of Organic and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: medicinal chemistry; organic synthesis; heterocycles; P-glycoprotein; anticancer; antimicrobials; chiral drugs; marine natural products
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Special Issue Information

Dear Colleagues,

We are pleased to announce that, as is the tradition with previous renditions of the Electronic Conference on Medicinal Chemistry (ECMC), we are launching a Special Issue in Pharmaceuticals to collect the most exciting contributions from this eighth ECMC.  The ECMC 2022 will be hosted on the online platform sciforum.net throughout the month of November. We have received a large number of outstanding contributions covering a wide variety of topics within the medicinal chemistry discipline. We invite authors to contribute a full article describing their original experimental results presented at the ECMC 2022.

Dr. Alfredo Berzal-Herranz
Dr. Maria Emília De Sousa
Guest Editors

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Published Papers (5 papers)

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Research

15 pages, 1888 KiB  
Article
Application of tris-(4,7-Diphenyl-1,10 phenanthroline)ruthenium(II) Dichloride to Detection of Microorganisms in Pharmaceutical Products
by Rafał Hałasa, Katarzyna Turecka, Magdalena Smoktunowicz, Urszula Mizerska and Czesława Orlewska
Pharmaceuticals 2023, 16(6), 856; https://doi.org/10.3390/ph16060856 - 08 Jun 2023
Cited by 2 | Viewed by 1143
Abstract
tris-[(4,7-diphenyl-1,10-phenanthroline)ruthenium(II)] dichloride (Ru(DPP)3Cl2), a fluorescent sensor which is sensitive to the amount of oxygen in the sample, was applied using the fluorescent optical respirometry (FOR) technique. The oxygen in the samples quenches the fluorescence. The fluorescence intensity depends [...] Read more.
tris-[(4,7-diphenyl-1,10-phenanthroline)ruthenium(II)] dichloride (Ru(DPP)3Cl2), a fluorescent sensor which is sensitive to the amount of oxygen in the sample, was applied using the fluorescent optical respirometry (FOR) technique. The oxygen in the samples quenches the fluorescence. The fluorescence intensity depends on the metabolic rate of the viable microorganisms. The effect of DMSO and plant extracts on bacteria was determined by FOR. It was shown that the MIC values obtained by FOR were consistent with the results of the MIC determinations using the method of serial dilutions; at the same time, the effects of concentrations lower than the growth-inhibitory concentrations on microbial cells were demonstrated. The FOR method enables the detection of multiplying bacteria in sterile and non-sterile pharmaceutical preparations in real time, which significantly shortens the time required to obtain results and allows the introduction of repair processes in the production. This method also allows for quick, unambiguous detection and the counting of the viable cells of aerobic microorganisms in non-sterile pharmaceuticals. Full article
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13 pages, 5686 KiB  
Article
Effect of the Composition of Leuzea and Cranberry Meal Extracts on Metabolic Processes in Norm and Pathology
by Daria Khalikova, Sergey An’kov, Nataliya Zhukova, Tatyana Tolstikova, Sergey Popov and Anastasia Saiko
Pharmaceuticals 2023, 16(5), 768; https://doi.org/10.3390/ph16050768 - 19 May 2023
Cited by 1 | Viewed by 1189
Abstract
This study was conducted to evaluate the effects of long-term administration of a new herbal composition of leuzea and cranberry meal extracts at a dose of 70:500 mg/kg in healthy and pathological mice. After 4 weeks of daily composition administration to healthy CD-1 [...] Read more.
This study was conducted to evaluate the effects of long-term administration of a new herbal composition of leuzea and cranberry meal extracts at a dose of 70:500 mg/kg in healthy and pathological mice. After 4 weeks of daily composition administration to healthy CD-1 mice and C57BL/6 mice with diet-induced metabolic syndrome, oral glucose tolerance test (OGTT), serum biochemical examination and histology of internal organs were performed. Additionally, histological examination of white and brown adipose tissue was performed to evaluate the ability of the composition to prevent abdominal obesity in C57BL/6Ay (agouti yellow) mice. The results showed that the composition increased tissue sensitivity to glucose in healthy CD-1 mice; at the same time, it did not worsen the course of pathological processes in pathological mice. In both cases, the application of the developed composition was safe and contributed to the restoration of metabolic parameters. Full article
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20 pages, 31817 KiB  
Article
Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen
by Nikola Nedeljković, Vladimir Dobričić, Jelena Bošković, Marina Vesović, Jovana Bradić, Marijana Anđić, Aleksandar Kočović, Nevena Jeremić, Jovana Novaković, Vladimir Jakovljević, Zorica Vujić and Miloš Nikolić
Pharmaceuticals 2023, 16(5), 666; https://doi.org/10.3390/ph16050666 - 28 Apr 2023
Cited by 6 | Viewed by 1474
Abstract
The aim of the study was a synthesis and investigation of the dose-dependent anti-inflammatory effect of new thiourea derivatives of naproxen with selected aromatic amines and esters of aromatic amino acids. The results of the in vivo study indicate that derivatives of m [...] Read more.
The aim of the study was a synthesis and investigation of the dose-dependent anti-inflammatory effect of new thiourea derivatives of naproxen with selected aromatic amines and esters of aromatic amino acids. The results of the in vivo study indicate that derivatives of m-anisidine (4) and N-methyl tryptophan methyl ester (7) showed the most potent anti-inflammatory activity four hours after injection of carrageenan, with the percentage of inhibition of 54.01% and 54.12%, respectively. In vitro assays of COX-2 inhibition demonstrated that none of the tested compounds achieved 50% inhibition at concentrations lower than 100 µM. On the other hand, the aromatic amine derivatives (15) accomplished significant inhibition of 5-LOX, and the lowest IC50 value was observed for compound 4 (0.30 μM). High anti-edematous activity of compound 4 in the rat paw edema model, together with potent inhibition of 5-LOX, highlight this compound as a promising anti-inflammatory agent. Full article
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18 pages, 1619 KiB  
Article
Synthesis, Evaluation of Enzyme Inhibition and Redox Properties of Potential Dual COX-2 and 5-LOX Inhibitors
by Jelena Bošković, Vladimir Dobričić, Marija Mihajlović, Jelena Kotur-Stevuljević and Olivera Čudina
Pharmaceuticals 2023, 16(4), 549; https://doi.org/10.3390/ph16040549 - 06 Apr 2023
Cited by 1 | Viewed by 1487
Abstract
Various dual inhibitors of COX-2 and 5-LOX enzymes have been developed so far in order to obtain more effective and safer anti-inflammatory drugs. The aim of this study was to design and synthesize new dual COX-2 and 5-LOX inhibitors, and to evaluate their [...] Read more.
Various dual inhibitors of COX-2 and 5-LOX enzymes have been developed so far in order to obtain more effective and safer anti-inflammatory drugs. The aim of this study was to design and synthesize new dual COX-2 and 5-LOX inhibitors, and to evaluate their enzyme inhibition potential and redox properties. Thirteen compounds (113) were designed taking into account structural requirements for dual COX-2 and 5-LOX inhibition and antioxidant activity, synthesized, and structurally characterized. These compounds can be classified as N-hydroxyurea derivatives (1, 2 and 3), 3,5-di-tert-butylphenol derivatives (4, 5, 6, 7 and 13), urea derivatives (8, 9 and 10) and “type B hydroxamic acids” (11 and 12). COX-1, COX-2 and 5-LOX inhibitory activities were evaluated using fluorometric inhibitor screening kits. The evaluation of the redox activity of newly synthesized compounds was performed in vitro in the human serum pool using redox status tests. The prooxidative score, the antioxidative score and the oxy-score were calculated. Seven out of thirteen synthesized compounds (1, 2, 3, 5, 6, 11 and 12) proved to be dual COX-2 and 5-LOX inhibitors. These compounds expressed good COX-2/COX-1 selectivity. Moreover, dual inhibitors 1, 3, 5, 11 and 12 showed good antioxidant properties. Full article
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15 pages, 6109 KiB  
Article
Characterization of URB Series Synthetic Cannabinoids by HRMS and UHPLC–MS/MS
by Marco Agostini, Donata Favretto, Caterina Renzoni, Susanna Vogliardi and Andrea Duranti
Pharmaceuticals 2023, 16(2), 201; https://doi.org/10.3390/ph16020201 - 29 Jan 2023
Cited by 2 | Viewed by 1915
Abstract
A large number of synthetic cannabinoids are included in new psychoactive substances (NPS) and constitute an open research area in analytical pharmaceutical and toxicology when methods are needed to unambiguously identify these substances and their metabolites in biological fluids. A full molecular characterization [...] Read more.
A large number of synthetic cannabinoids are included in new psychoactive substances (NPS) and constitute an open research area in analytical pharmaceutical and toxicology when methods are needed to unambiguously identify these substances and their metabolites in biological fluids. A full molecular characterization of five synthetic molecules of the URB series that is able to interact with the endocannabinoid system was achieved with a high-resolution mass spectrometry (HRMS) in positive ion electrospray ionization and collisional experiments on the protonated parent ions, obtaining characteristic fragmentation patterns. Ultra-high-performance liquid chromatography coupled with a triple quadrupole (UHPLC-MS/MS) has also been used, which can help develop methods for screening and confirming synthetic cannabinoids in biological fluids. Full article
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