Special Issue "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: 26 January 2024 | Viewed by 1388

Special Issue Editors

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

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Keywords

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

Published Papers (1 paper)

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Research

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
Pharmaceuticals 2023, 16(6), 804; https://doi.org/10.3390/ph16060804 - 29 May 2023
Cited by 1 | Viewed by 1138
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 3a3o. 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 3a3o. The compounds were obtained with good yields of pyrrolo[3,4-c]pyrrole scaffold 2a2c 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
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