The 20th Anniversary of Pharmaceuticals—New Insights in Medicinal Chemistry of Nitrogen-Containing Compounds

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: 25 July 2024 | Viewed by 1270

Special Issue Editors


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Guest Editor
Department of Organic Chemistry, University of Vigo, Vigo, Spain
Interests: rational drug design; small heterocyclic compounds; enzyme inhibitors; hybrid compounds; nucleoside analogues; ageing-related diseases

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Guest Editor
Department of Organic Chemistry, Universidade de Vigo, Vigo, Spain
Interests: nucleoside analogues; lysosomal storage diseases; heterocyclic compounds; drug synthesis; drug design; enzyme inhibition

Special Issue Information

Dear Colleagues,

Nitrogen atoms are very important elements in life. Together with carbon, oxygen, and hydrogen, they are part of essential biomolecules, such as nucleic acids, proteins, enzymes, vitamins, hormones, and numerous secondary metabolites of both animal and plant kingdoms.

Nitrogen-containing scaffolds of acyclic or cyclic structure have made valuable contributions to medicinal chemistry, providing a rich diversity source for drug design. Its ability to display a moldable acid–base behavior and establish diverse supramolecular interactions, including electrostatic forces, conventional and unconventional hydrogen interactions, van der Waals and hydrophobic bonds, or even π-π interactions, allows them to bind to a wide variety of drug targets.

Among nitrogen-based frameworks, it is noteworthy that heterocyclic systems are the most prevalent for the design of pharmacophores due to their heterogeneous structure and biological significance. Azoles, azines, and azepines of monocyclic or bicyclic structure are currently recognized as indispensable building blocks for the development of novel therapeutic agents with a wide spectrum of biological effects. These ring systems are present in many FDA-approved drugs which are effective for the treatment of several diseases.

In addition, nitrogen derivatives such as urea, thiourea, guanidine, sulphonamide, propargylamine, and nitro-containing compounds are also acknowledged as privileged structural motifs in medicinal and synthetic chemistry. Other nitrogen functional groups which have recently emerged as unconventional pharmacophores include isocyanides and sulfoximines, which are two strategic moieties used for drug design purposes because of their interesting properties (including favorable physicochemical and metabolic behavior as well as good metal coordinative abilities, i.e., features associated with biological effects).  

This Special Issue of the journal Pharmaceuticals is devoted to new insights centered around the medicinal chemistry of nitrogen-containing compounds and invites both research papers and reviews on the use of acyclic and cyclic nitrogen scaffolds in drug design and development. This Special Issue aims to check the state of the art and describe the latest advances and the future prospects on this topic.

Prof. Dr. María del Carmen Terán Moldes
Prof. Dr. Pedro Besada Pereira
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

  • drug design
  • synthesis
  • nitrogen heterocycles
  • nitrogen functional groups
  • biological activity
  • structure-activity relationship
  • molecular modeling

Published Papers (1 paper)

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Research

19 pages, 5486 KiB  
Article
N-(coumarin-3-yl)cinnamamide Promotes Immunomodulatory, Neuroprotective, and Lung Function-Preserving Effects during Severe Malaria
by Paulo Gaio, Allysson Cramer, Natália Fernanda de Melo Oliveira, Samuel Porto, Lucas Kramer, Rayane Aparecida Nonato Rabelo, Rafaela das Dores Pereira, Laura Lis de Oliveira Santos, César Luís Nascimento Barbosa, Fabrício Marcus Silva Oliveira, Mauro Martins Teixeira, Remo Castro Russo, Maria João Matos and Fabiana Simão Machado
Pharmaceuticals 2024, 17(1), 46; https://doi.org/10.3390/ph17010046 - 27 Dec 2023
Viewed by 1091
Abstract
Plasmodium berghei ANKA (PbA) infection in mice resembles several aspects of severe malaria in humans, such as cerebral malaria and acute respiratory distress syndrome. Herein, the effects of N-(coumarin-3-yl)cinnamamide (M220) against severe experimental malaria have been investigated. Treatment with M220 proved to [...] Read more.
Plasmodium berghei ANKA (PbA) infection in mice resembles several aspects of severe malaria in humans, such as cerebral malaria and acute respiratory distress syndrome. Herein, the effects of N-(coumarin-3-yl)cinnamamide (M220) against severe experimental malaria have been investigated. Treatment with M220 proved to protect cognitive abilities and lung function in PbA-infected mice, observed by an object recognition test and spirometry, respectively. In addition, treated mice demonstrated decreased levels of brain and lung inflammation. The production and accumulation of microglia, and immune cells that produce the inflammatory cytokines TNF and IFN-γ, decreased, while the production of the anti-inflammatory cytokine IL-10 by innate and adaptive immune cells was enhanced. Treatment with M220 promotes immunomodulatory, neuroprotective, and lung function-preserving effects during experimental severe malaria. Therefore, it may be an interesting therapeutic candidate to treat severe malaria effects. Full article
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