molecules-logo

Journal Browser

Journal Browser

Ultimate Insight into the COX Inhibition

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (5 September 2021) | Viewed by 5318

Special Issue Editors


E-Mail Website
Guest Editor
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampl. Polifunzionale, Via P. Bucci, 87036 Arcavacata di Rende, Italy
Interests: drug design; small molecules; natural compounds; protein targeting; anticancer; antiviral; metabolic disorders
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Università della Calabria, Cosenza, Italy
Interests: computer aided drug design, synthesis and biological evaluation of heterocyclic small molecules as potential antiviral and anticancer drugs

Special Issue Information

Dear Colleagues,

Non-steroidal analgetics find a wide range of applications due to their high efficacy and largely manageable unwanted effects. The identification and functional definition of COX-1 and COX-2 isozymes, the main targets of these drugs, have contributed to stimulate research in this field. The search of new active molecules and the study of handy drug-releasing devices are currently compelling goals in this area, while addressing the action of a drug by the attribution of peculiar pharmacokinetic properties and the design of innovative light-protected pharmaceutical forms represent two new aspects widely investigated.  

This Special Issue aims to highlight the current efforts in pharmaceutical chemistry and pharmacology towards innovative strategies against inflammation. It welcomes works on advanced drug discovery approaches by in silico identification of alternative natural and synthetic COX ligands and on the study of structure–activity relationships and the design of convenient methods for the synthesis of effective agents. Nanotechnology applications and biological evaluation of anti-inflammatory therapies will be considered as well.

Dr. Fedora Grande
Prof. Dr. Antonio Garofalo
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

  • Natural and synthetic compounds
  • Drug design
  • Drug synthesis
  • Pharmacophore modelling and dynamic simulations
  • Structure–activity relationships
  • Target validation
  • Metabolic activation
  • Hit discovery
  • Hit-to-lead optimization
  • Analytical techniques and methodologies
  • Supramolecular chemistry
  • Biological evaluation
  • Photo-protective systems

Published Papers (2 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Jump to: Review

18 pages, 3811 KiB  
Article
Toward Multitasking Pharmacological COX-Targeting Agents: Non-Steroidal Anti-Inflammatory Prodrugs with Antiproliferative Effects
by Fedora Grande, Francesca Giordano, Maria Antonietta Occhiuzzi, Carmine Rocca, Giuseppina Ioele, Michele De Luca, Gaetano Ragno, Maria Luisa Panno, Bruno Rizzuti and Antonio Garofalo
Molecules 2021, 26(13), 3940; https://doi.org/10.3390/molecules26133940 - 28 Jun 2021
Cited by 7 | Viewed by 2053
Abstract
The antitumor activity of certain anti-inflammatory drugs is often attributed to an indirect effect based on the inhibition of COX enzymes. In the case of anti-inflammatory prodrugs, this property could be attributed to the parent molecules with mechanism other than COX inhibition, particularly [...] Read more.
The antitumor activity of certain anti-inflammatory drugs is often attributed to an indirect effect based on the inhibition of COX enzymes. In the case of anti-inflammatory prodrugs, this property could be attributed to the parent molecules with mechanism other than COX inhibition, particularly through formulations capable of slowing down their metabolic conversion. In this work, a pilot docking study aimed at comparing the interaction of two prodrugs, nabumetone (NB) and its tricyclic analog 7-methoxy-2,3-dihydro-1H-cyclopenta[b]naphthalen-1-one (MC), and their common active metabolite 6-methoxy-2-naphthylacetic acid (MNA) with the COX binding site, was carried out. Cytotoxicity, cytofluorimetry, and protein expression assays on prodrugs were also performed to assess their potential as antiproliferative agents that could help hypothesize an effective use as anticancer therapeutics. Encouraging results suggest that the studied compounds could act not only as precursors of the anti-inflammatory metabolite, but also as direct antiproliferative agents. Full article
(This article belongs to the Special Issue Ultimate Insight into the COX Inhibition)
Show Figures

Figure 1

Review

Jump to: Research

12 pages, 781 KiB  
Review
Photodegradation of Anti-Inflammatory Drugs: Stability Tests and Lipid Nanocarriers for Their Photoprotection
by Giuseppina Ioele, Fedora Grande, Michele De Luca, Maria Antonietta Occhiuzzi, Antonio Garofalo and Gaetano Ragno
Molecules 2021, 26(19), 5989; https://doi.org/10.3390/molecules26195989 - 02 Oct 2021
Cited by 14 | Viewed by 2611
Abstract
The present paper provides an updated overview of the methodologies applied in photodegradation studies of non-steroidal anti-inflammatory drugs. Photostability tests, performed according to international standards, have clearly demonstrated the photolability of many drugs belonging to this class, observed during the preparation of commercial [...] Read more.
The present paper provides an updated overview of the methodologies applied in photodegradation studies of non-steroidal anti-inflammatory drugs. Photostability tests, performed according to international standards, have clearly demonstrated the photolability of many drugs belonging to this class, observed during the preparation of commercial forms, administration or when dispersed in the environment. The photodegradation profile of these drugs is usually monitored by spectrophotometric or chromatographic techniques and in many studies the analytical data are processed by chemometric procedures. The application of multivariate analysis in the resolution of often-complex data sets makes it possible to estimate the pure spectra of the species involved in the degradation process and their concentration profiles. Given the wide use of these drugs, several pharmaceutical formulations have been investigated to improve their photostability in solution or gel, as well as the pharmacokinetic profile. The use of lipid nanocarriers as liposomes, niosomes or solid lipid nanoparticles has demonstrated to both minimize photodegradation and improve the controlled release of the entrapped drugs. Full article
(This article belongs to the Special Issue Ultimate Insight into the COX Inhibition)
Show Figures

Graphical abstract

Back to TopTop