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Pharmaceuticals
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Pharmaceuticals 2024—Recent Advances in Pharmaceutical Sciences Towards a Healthy Life
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Pharmaceuticals 2024—Recent Advances in Pharmaceutical Sciences Towards a Healthy Life

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

Deadline for manuscript submissions: 31 May 2025 | Viewed by 5729

Special Issue Editors

Prof. Dr. Amélia Pilar Rauter

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Guest Editor
Departamento de Química e Bioquímica (DQB) e Centro de Química Estrutural (CQE), Institute of Molecular Sciences, Faculdade de Ciências, Universidade de Lisboa, Lisboa, Portugal
Interests: neurodegenerative diseases; organic synthesis; natural products; antibiotics; antidiabetics; carbohydrate chemistry
Special Issues, Collections and Topics in MDPI journals
Dr. Alfredo Berzal-Herranz

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Guest Editor
Department of Molecular Biology, Instituto de Parasitología y Biomedicina López-Neyra (IPBLN) CSIC, Granada, Spain
Interests: antisense; aptamers; RNA virus; genomic RNAs; HCV genome; HIV genome; structure/function of RNA domains; coronavirus
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Mary J. Meegan

E-Mail Website
Guest Editor
School of Pharmacy and Pharmaceutical Sciences, Trinity Biomedical Sciences Institute, Trinity College Dublin, 152−160 Pearse Street, D02 R590 Dublin, Ireland
Interests: drug development; antiestrogens; in silico; breast cancer; design and synthesis; synthetic methods; amphetamines; anticancer drug design; carbapenem antibiotics; chemistry of drug metabolism; chemistry of drug receptor interactions; design and synthesis of drugs; molecular modelling of estrogen receptor antagonists; pharmacologically active heterocycles
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue is related to the conference “Pharmaceuticals 2024—Recent Advances in Pharmaceutical Sciences Towards a Healthy Life”, which will be held in Barcelona, Spain, 27–29 November 2024.

Covering the newest technologies and the research areas of medicinal chemistry, natural products, organic synthesis, radiopharmaceuticals, pharmacology, toxicology, and biomolecular and glycosciences, among others, the meeting will bring experts together to present their latest findings on relevant topics such as combating infection, inflammation, pain, and neurodegeneration.

In this meeting, we encourage participation from all areas of pharmaceutical research to highlight recent advances in the field of applied chemistry in the search for novel solutions to global pharmaceutical challenges. This conference will provide the opportunity to finally meet in person and bring together younger researchers, experts, and industry to plan science and technology for the future. A roundtable will be organized to start and facilitate further discussions.

Conference participants, as well as all researchers working in the field, are invited to contribute original research papers or reviews to this Special Issue of Pharmaceuticals.

Prof. Dr. Amélia Pilar Rauter
Dr. Alfredo Berzal-Herranz
Prof. Dr. Mary J. Meegan
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 submissions that pass pre-check are 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. Pharmaceuticals 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 2900 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

  • medicinal chemistry
  • natural products
  • organic synthesis
  • radiopharmaceuticals
  • pharmacology
  • toxicology
  • glycosciences

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (5 papers)

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Research

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9 pages, 892 KiB  
Article
Sacubitril Does Not Exert Proarrhythmic Effects in Combination with Different Antiarrhythmic Drugs
by Christian Ellermann, Carlo Mengel, Julian Wolfes, Felix K. Wegner, Benjamin Rath, Julia Köbe, Lars Eckardt and Gerrit Frommeyer
Pharmaceuticals 2025, 18(2), 230; https://doi.org/10.3390/ph18020230 - 8 Feb 2025
Viewed by 629
Abstract
Background: Previous studies suggest a direct effect of sacubitril on cardiac electrophysiology and indicate potential arrhythmic interactions between sacubitril and antiarrhythmic drugs. Therefore, the aim of this study was to explore the electrophysiologic effects of combining sacubitril with the antiarrhythmic drugs d,l-sotalol and [...] Read more.
Background: Previous studies suggest a direct effect of sacubitril on cardiac electrophysiology and indicate potential arrhythmic interactions between sacubitril and antiarrhythmic drugs. Therefore, the aim of this study was to explore the electrophysiologic effects of combining sacubitril with the antiarrhythmic drugs d,l-sotalol and mexiletine in isolated hearts. Methods and results: A total of 25 rabbit hearts were perfused using a Langendorff setup. Following baseline data collection, hearts were treated with mexiletine (25 µM, 13 hearts) or d,l-sotalol (100 µM, 12 hearts). Monophasic action potential demonstrated an abbreviation of action potential duration (APD90) after administration of mexiletine. Spatial dispersion of repolarization remained unchanged after mexiletine treatment, whereas effective refractory periods (ERP) were significantly prolonged. D,l-sotalol prolonged cardiac repolarization and amplified spatial dispersion. Further infusion of sacubitril (5 µM) led to a significant reduction in APD90 and ERP in the mexiletine group. In the d,l-sotalol group, additional administration of sacubitril shortened cardiac repolarization duration without affecting spatial dispersion. No proarrhythmic effect was observed after mexiletine treatment as assessed by a predefined pacing protocol. Additional sacubitril treatment did not increase ventricular vulnerability. When potassium concentration was reduced, 30 episodes of torsade de pointes tachycardia occurred after d,l-sotalol treatment. Additional sacubitril treatment significantly suppressed torsade de pointes tachycardia (eight episodes) in the d,l-sotalol-group. Conclusions: In class IB- and class III-pretreated hearts, sacubitril shortened refractory periods and cardiac repolarization duration. The combination of sacubitril with the antiarrhythmic drugs d,l-sotalol and mexiletine demonstrates a safe electrophysiologic profile and sacubitril reduces the occurrence of class III-related proarrhythmia, i.e., torsade de pointes tachycardia. Full article
(This article belongs to the Special Issue Pharmaceuticals 2024—Recent Advances in Pharmaceutical Sciences Towards a Healthy Life)
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15 pages, 1431 KiB  
Article
Anticoagulant Management After Emergency Surgery or Major Bleeding in Anticoagulated Patients—Results of the Prospective RADOA Registry
by Jana Last, Ingvild Birschmann, Simone Lindau, Stavros Konstantinides, Oliver Grottke, Ulrike Nowak-Göttl, Barbara Zydek, Christian von Heymann, Jan Beyer-Westendorf, Sebastian Schellong, Patrick Meybohm, Andreas Greinacher, Eva Herrmann and Edelgard Lindhoff-Last
Pharmaceuticals 2025, 18(2), 170; https://doi.org/10.3390/ph18020170 - 26 Jan 2025
Viewed by 1080
Abstract
Background: Major bleeding or emergency surgery are the most frequently observed emergency situations in patients anticoagulated with vitamin K antagonists (VKAs) or direct oral anticoagulants (DOACs). The restart of anticoagulation after these situations is a therapeutic dilemma. Methods: The prospective RADOA registry is [...] Read more.
Background: Major bleeding or emergency surgery are the most frequently observed emergency situations in patients anticoagulated with vitamin K antagonists (VKAs) or direct oral anticoagulants (DOACs). The restart of anticoagulation after these situations is a therapeutic dilemma. Methods: The prospective RADOA registry is an observational, noninterventional multicenter registry that documents the management of severe bleeding or emergency surgery in patients treated with VKAs or DOACs. In this substudy, we analyzed time point, type, and dosage of anticoagulant resumption after emergency situations. Results: Overall, 78 emergency surgery patients and 193 major bleeding patients were analyzed. Median age was similar in the VKA- and DOAC-treated groups (emergency surgery: 77 years, major bleeding: 79 years). Anticoagulants were restarted significantly earlier after emergency surgery compared to major bleeding, with no difference between the VKA and DOAC groups. While patients after cardiothoracic surgery received UFH intravenously, patients with trauma or having received abdominal surgery were mainly treated with prophylactic LMWH s.c.. After major bleeding, the majority of patients were treated with prophylactic LMWH. None of the patients in the emergency surgery group and 17% (4/24) of the major bleeding group with recurrent bleeding (12%, 24/193) experienced recurrent bleeding after restart of anticoagulation. Thromboembolism occurred rarely in both patient groups (emergency surgery: 3%, major bleeding 4%). Conclusions: Time points of restart, type, and dosage of anticoagulants are highly diverse in this high-risk patient population. Resumption of prophylactic anticoagulation is associated with a low risk of thrombosis and should be initiated as soon as possible. Full article
(This article belongs to the Special Issue Pharmaceuticals 2024—Recent Advances in Pharmaceutical Sciences Towards a Healthy Life)
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Review

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23 pages, 1056 KiB  
Review
Small Molecules in the Treatment of Acute Severe Ulcerative Colitis: A Review of Current Evidence
by Raffaele Pellegrino, Giuseppe Imperio, Ilaria De Costanzo, Michele Izzo, Fabio Landa, Assunta Tambaro, Antonietta Gerarda Gravina and Alessandro Federico
Pharmaceuticals 2025, 18(3), 308; https://doi.org/10.3390/ph18030308 - 23 Feb 2025
Viewed by 768
Abstract
Ulcerative colitis (UC) is an inflammatory bowel disease in which one-quarter of patients are at risk of developing a severe form of the disease known as acute severe UC (ASUC). This condition exposes patients to serious complications, including toxic megacolon, surgical intervention, and [...] Read more.
Ulcerative colitis (UC) is an inflammatory bowel disease in which one-quarter of patients are at risk of developing a severe form of the disease known as acute severe UC (ASUC). This condition exposes patients to serious complications, including toxic megacolon, surgical intervention, and even death. The current therapeutic strategy relies on time-dependent, multi-step algorithms that integrate systemic corticosteroids, calcineurin inhibitors, and biologic agents (specifically infliximab) as medical therapy aimed at avoiding colectomy. Despite this approach, a significant proportion of patients fail to respond to either corticosteroids or infliximab and may require alternative therapeutic options if there is no urgent surgical necessity. These alternatives include other biologics or emerging small molecules, although the evidence supporting these treatments remains extremely low, even considering their well-documented and promising efficacy and safety in moderate-to-severe UC. Conversely, it is necessary to investigate whether infliximab can be effectively replaced or surpassed by other approved biological agents and small molecules as first-line therapy after steroid resistance. This review aims to summarise the available evidence on small molecules, specifically Janus kinase inhibitors and sphingosine-1-phosphate receptor modulators. Full article
(This article belongs to the Special Issue Pharmaceuticals 2024—Recent Advances in Pharmaceutical Sciences Towards a Healthy Life)
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26 pages, 1298 KiB  
Review
Drug Treatment Direction Based on the Molecular Mechanism of Breast Cancer Brain Metastasis
by Yumin Zhang, Haotian Shang, Jiaxuan Zhang, Yizhi Jiang, Jiahao Li, Huihua Xiong and Tengfei Chao
Pharmaceuticals 2025, 18(2), 262; https://doi.org/10.3390/ph18020262 - 16 Feb 2025
Viewed by 823
Abstract
Today, breast cancer (BC) is the most frequently diagnosed malignancy and a leading cause of cancer-related deaths among women worldwide. Brain metastases (BMs) are a common complication among individuals with advanced breast cancer, significantly impacting both survival rates and the overall condition of [...] Read more.
Today, breast cancer (BC) is the most frequently diagnosed malignancy and a leading cause of cancer-related deaths among women worldwide. Brain metastases (BMs) are a common complication among individuals with advanced breast cancer, significantly impacting both survival rates and the overall condition of life of patients. This review systematically analyzes the innovative approaches to drug treatment for breast cancer brain metastases (BCBMs), with particular emphasis placed on treatments targeting molecular mechanisms and signaling pathways and drug delivery strategies targeting the blood brain barrier (BBB). The article discusses various drugs that have demonstrated effectiveness against BCBM, featuring a mix of monoclonal antibodies, nimble small-molecule tyrosine kinase inhibitors (TKIs), and innovative antibody-drug conjugates (ADCs). This study of various drugs and techniques designed to boost the permeability of the BBB sheds light on how these innovations can improve the treatment of brain metastases. This review highlights the need to develop new therapies for BCBM and to optimize existing treatment strategies. With a deeper comprehension of the intricate molecular mechanisms and advances in drug delivery technology, it is expected that more effective personalized treatment options will become available in the future for patients with BCBM. Full article
(This article belongs to the Special Issue Pharmaceuticals 2024—Recent Advances in Pharmaceutical Sciences Towards a Healthy Life)
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26 pages, 2595 KiB  
Review
Mechanisms of Copper-Induced Autophagy and Links with Human Diseases
by Yuanyuan Fu, Shuyan Zeng, Zhenlin Wang, Huiting Huang, Xin Zhao and Min Li
Pharmaceuticals 2025, 18(1), 99; https://doi.org/10.3390/ph18010099 - 15 Jan 2025
Viewed by 1036
Abstract
As a structural and catalytic cofactor, copper is involved in many biological pathways and is required for the biochemistry of all living organisms. However, excess intracellular copper can induce cell death due to its potential to catalyze the generation of reactive oxygen species, [...] Read more.
As a structural and catalytic cofactor, copper is involved in many biological pathways and is required for the biochemistry of all living organisms. However, excess intracellular copper can induce cell death due to its potential to catalyze the generation of reactive oxygen species, thus copper homeostasis is strictly regulated. And the deficiency or accumulation of intracellular copper is connected with various pathological conditions. Since the success of platinum-based compounds in the clinical treatment of various types of neoplasias, metal-based drugs have shown encouraging perspectives for drug development. Compared to platinum, copper is an essential intracellular trace element that may have better prospects for drug development than platinum. Recently, the potential therapeutic role of copper-induced autophagy in chronic diseases such as Parkinson’s, Wilson’s, and cardiovascular disease has already been demonstrated. In brief, copper ions, numerous copper complexes, and copper-based nano-preparations could induce autophagy, a lysosome-dependent process that plays an important role in various human diseases. In this review, we not only focus on the current advances in elucidating the mechanisms of copper or copper-based compounds/preparations on the regulation of autophagy but also outline the association between copper-induced autophagy and human diseases. Full article
(This article belongs to the Special Issue Pharmaceuticals 2024—Recent Advances in Pharmaceutical Sciences Towards a Healthy Life)
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