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Adenosine Receptor Antagonists: Design, Synthesis and Biochemical Analyses

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (30 June 2024) | Viewed by 882

Special Issue Editors


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Guest Editor
Medicinal Chemistry Unit, School of Pharmacy, University of Camerino, Via Madonna delle Carceri, 62032 Camerino, Italy
Interests: G-protein coupled receptors; P1 adenosine receptr agonists and antagonists; P2 ligands; antitumor drugs; enzyme inhibitors; medicinal chemistry

E-Mail Website
Guest Editor
Medicinal Chemistry Unit, School of Pharmacy, University of Camerino, Via Madonna delle Carceri, 62032 Camerino, Italy
Interests: adenosine receptor antagonists; neuroinflammation

Special Issue Information

Dear Colleagues,

It is a pleasure for me to invite you to submit your research results in the field of the medicinal chemistry of the adenosinergic system.

Adenosine (Ado) is an extracellular natural autacoid product of nucleotide metabolism, such as in ATP and ADP, and mediates a wide range of events under normal and pathological conditions. Adenosine receptors (ARs) belong to the G-coupled signalling receptors and are divided into four subtypes (A1, A2A, A2B, and A3). These receptors are broadly expressed in the central and peripheral nervous systems and are also present in nearly all organs and tissues, modulating cardiovascular and respiratory activity, the immune systems, and a wide variety of physiological processes. Furthermore, ARs play an important role in several pathologies, leading to the consideration of this receptor system as a potential therapeutic target in a variety of pathological conditions, such as neurological disorders, cardiovascular diseases, cancer, and inflammatory as well as autoimmune diseases.

This Special Issue aims to provide the research community with recent advances in the field of AR antagonists as targets in human disease. Topics include novel AR antagonists and AR allosteric modulators as promising tools and diagnostic probes, including their molecular modelling, synthesis, biological evaluation, and pharmacokinetic properties. Authors are invited to submit original articles dealing with their research in this area of investigation. Review articles summarizing the current knowledge on adenosine receptors and their antagonists will also be of interest.

Dr. Gabriella Marucci
Dr. Michela Buccioni
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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

  • adenosine receptors
  • adenosine receptor antagonists
  • heterocyclic compounds
  • medicinal chemistry
  • adenosine receptor ligands
  • molecular modelling
  • synthesis of adenosine receptor antagonists
  • pharmacokinetic properties
  • pharmacological tool
  • diagnostic probes

Published Papers (1 paper)

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Research

17 pages, 1675 KiB  
Article
2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives
by Filipe Areias, Carla Correia, Ashly Rocha, Sofia Teixeira, Marián Castro, Jose Brea, Huabin Hu, Jens Carlsson, Maria I. Loza, M. Fernanda Proença and M. Alice Carvalho
Molecules 2024, 29(11), 2543; https://doi.org/10.3390/molecules29112543 - 28 May 2024
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Abstract
A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A1, A2A, A2B, and A3 adenosine receptor subtypes. Eleven purines showed potent antagonism at A1, A3 [...] Read more.
A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A1, A2A, A2B, and A3 adenosine receptor subtypes. Eleven purines showed potent antagonism at A1, A3, dual A1/A2A, A1/A2B, or A1/A3 adenosine receptors. Additionally, three compounds showed high affinity without selectivity for any specific adenosine receptor. The structure-activity relationships were made for this group of new compounds. The 9-methylpurine derivatives were generally less potent but more selective, and the 9H-purine derivatives were more potent but less selective. These compounds can be an important source of new biochemical tools and/or pharmacological drugs. Full article
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