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Pharmaceuticals
Special Issues
Design, Synthesis and Biological Evaluation with Potential Anti-inflammatory Activity
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Design, Synthesis and Biological Evaluation with Potential Anti-inflammatory Activity

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

Deadline for manuscript submissions: 22 December 2024 | Viewed by 3536

Special Issue Editors

Dr. Berenika M. Szczȩśniak-Siȩga

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Guest Editor
Department of Medicinal Chemistry, Faculty of Pharmacy, Wroclaw Medical University, 50-367 Wrocław, Poland
Interests: synthesis; 1,2-benzothiazine; oxicams; anti-inflammatory; chemoprevention; cancer
Dr. Żaneta Czyżnikowska

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Guest Editor
Department of Basic Chemical Sciences, Faculty of Pharmacy, Wroclaw Medical University, 50-367 Wrocław, Poland
Interests: molecular modeling; anti-inflammatory drugs; drug design
Special Issues, Collections and Topics in MDPI journals
Dr. Aleksandra Redzicka

E-Mail Website
Guest Editor
Department of Medicinal Chemistry, Faculty of Pharmacy, Wroclaw Medical University, 50-367 Wrocław, Poland
Interests: synthesis; pyrrolopyrrole; pyridazines; cyclic imides; anti-inflammatory activity; analgesic activity

Special Issue Information

Dear Colleagues,

Inflammation is a kind of defensive body reaction in response to damaging factors. Cells of the immune system, connective tissue cells, some blood proteins, and blood vessels are involved in the inflammatory reaction. The purpose of inflammation is to limit the harmful factor, neutralize it and repair damaged tissues. Sometimes, the immune response is inappropriately intensified in relation to the damaging stimulus or is directed against healthy tissues.

Many studies have shown that the inflammatory process is involved in the initiation and progression of many diseases, such as asthma, rheumatoid arthritis, cardiovascular disorders, diabetes, Crohn's disease, multiple sclerosis, neurogenerative disorders such as Alzheimer's disease, and even cancer. Inflammatory diseases are a widespread medical, social, and economic burden, and their pharmacotherapy is still an unresolved problem. Therefore, there is a great and urgent need to develop anti-inflammatory drugs with new mechanisms of action.

Research in recent years has shown that very different signaling pathways are associated with the initiation and progression of inflammation. The classical inflammatory pathways are IL-6/JAK/STAT3, p38 MAPK, and PI3K, and non-classical ones include  Hippo. Recently, the Hippo pathway has been linked to various inflammatory modulators such as TNF-α, IL-6, COX-2, HIF-1α, AP-1, JAK, and STAT. In addition to searching for compounds with innovative anti-inflammatory mechanisms, it is also worth continuing research on compounds with anti-inflammatory effects that are associated with blocking COX/LOX enzymes and multi-target drug design.

The purpose of this Special Issue is to gather original and review articles presenting data on the design, synthesis, pharmacological research, and molecular modeling of new compounds with potential anti-inflammatory activity.

Dr. Berenika M. Szczȩśniak-Siȩga
Dr. Żaneta Czyżnikowska
Dr. Aleksandra Redzicka
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

  • anti-inflammatory
  • COX/LOX
  • IL-6
  • JAK
  • STAT3
  • p38MAPK
  • TNF-α
  • asthma
  • Alzheimer's disease
  • cancer

Published Papers (2 papers)

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Research

12 pages, 2060 KiB  
Article
Total Synthesis and Anti-Inflammatory Evaluation of Osajin, Scandenone and Analogues
by Rui Wang, Ran Ma, Ke Feng, Hongchen Lu, Wei Zhao and Hongzhen Jin
Pharmaceuticals 2024, 17(1), 86; https://doi.org/10.3390/ph17010086 - 9 Jan 2024
Cited by 2 | Viewed by 1058
Abstract
In this study, the total synthesis of osajin, scandenone and their analogues have been accomplished. The key synthetic steps include aldol/intramolecular iodoetherification/elimination sequence reactions and a Suzuki coupling reaction to assemble the tricyclic core, chemoselective propargylation and Claisen rearrangement reactions to obtain natural [...] Read more.
In this study, the total synthesis of osajin, scandenone and their analogues have been accomplished. The key synthetic steps include aldol/intramolecular iodoetherification/elimination sequence reactions and a Suzuki coupling reaction to assemble the tricyclic core, chemoselective propargylation and Claisen rearrangement reactions to obtain natural compounds. In addition, we also designed and synthesized twenty-five natural product analogues. All synthetic compounds were screened for anti-inflammatory activity against tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. Collectively, Compound 39e and 39d were considered as promising lead compounds for further development. Full article
(This article belongs to the Special Issue Design, Synthesis and Biological Evaluation with Potential Anti-inflammatory Activity)
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26 pages, 9608 KiB  
Article
Design, Synthesis, Biological Evaluation, and Molecular Docking Study of 4,6-Dimethyl-5-aryl/alkyl-2-[2-hydroxy-3-(4-substituted-1-piperazinyl)propyl]pyrrolo[3,4-c]pyrrole-1,3(2H,5H)-diones as Anti-Inflammatory Agents with Dual Inhibition of COX and LOX
by Aleksandra Redzicka, Benita Wiatrak, Izabela Jęśkowiak-Kossakowska, Andrzej Kochel, Remigiusz Płaczek and Żaneta Czyżnikowska
Pharmaceuticals 2023, 16(6), 804; https://doi.org/10.3390/ph16060804 - 29 May 2023
Cited by 3 | Viewed by 2043
Abstract
In the present study, we characterize the biological activity of a newly designed and synthesized series of 15 compounds 2-[2-hydroxy-3-(4-substituted-1-piperazinyl)propyl] derivatives of pyrrolo[3,4-c]pyrrole 3a–3o. The compounds were obtained with good yields of pyrrolo[3,4-c]pyrrole scaffold 2a– [...] Read more.
In the present study, we characterize the biological activity of a newly designed and synthesized series of 15 compounds 2-[2-hydroxy-3-(4-substituted-1-piperazinyl)propyl] derivatives of pyrrolo[3,4-c]pyrrole 3a–3o. The compounds were obtained with good yields of pyrrolo[3,4-c]pyrrole scaffold 2a–2c with secondary amines in C2H5OH. The chemical structures of the compounds were characterized by 1H-NMR, 13C-NMR, FT-IR, and MS. All the new compounds were investigated for their potencies to inhibit the activity of three enzymes, i.e., COX-1, COX-2, and LOX, by a colorimetric inhibitor screening assay. In order to analyze the structural basis of interactions between the ligands and cyclooxygenase/lipooxygenase, experimental data were supported by the results of molecular docking simulations. The data indicate that all of the tested compounds influence the activity of COX-1, COX-2, and LOX. Full article
(This article belongs to the Special Issue Design, Synthesis and Biological Evaluation with Potential Anti-inflammatory Activity)
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