Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
7.3
4.3
Journals
Antibiotics
Special Issues
New Insights into Antimicrobial Compounds: From Synthesis and Discovery to...
share announcement

New Insights into Antimicrobial Compounds: From Synthesis and Discovery to Mechanisms of Action

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Mechanisms and Structural Biology of Antibiotic Action".

Deadline for manuscript submissions: 15 September 2024 | Viewed by 1330

Special Issue Editor

Prof. Dr. Rosane Nassar Meireles Guerra

E-Mail Website
Guest Editor
Laboratory of Immunophysiolgy, Federal University of Maranhão, São Luís 65080-805, Brazil
Interests: antimicrobial; drug discovery; inflammation

Special Issue Information

Dear Colleagues,

Infections, caused by drug-resistant and/or slow-growing bacteria, increasingly represent some of the greatest challenges facing health organizations worldwide. The decreased efficacy of the large percentage of antimicrobials currently in clinical use against these types of infections emphasizes the need for the development of novel antimicrobial agents that will be effective in eradicating a broad spectrum of bacteria, regardless of their cell cycle stage.

This Special Issue aims to collect papers describing novel compounds with antimicrobial effects, whether from synthesis or natural sources. We also welcome papers describing the discovery of novel targets and molecular mechanisms of action, as well as on the application of omics and bioinformatic tools to antimicrobial drug discovery pathways.

Prof. Dr. Rosane Nassar Meireles Guerra
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at mdpi.longhoe.net 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. Antibiotics 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.

Prof. Dr. Rosane Nassar Meireles Guerra
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at mdpi.longhoe.net 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. Antibiotics 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

  • antimicrobial
  • drug discovery
  • synthetic methods
  • natural sources
  • antimicrobial targets
  • mechanisms of action
  • omics tools

Published Papers (1 paper)

Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:

Research

14 pages, 3098 KiB  
Article
Evaluation of the Antibacterial Effect of Aurone-Derived Triazoles on Staphylococcus aureus
by Csilla Klara Szepe, Arjun Kafle, Shrijana Bhattarai, Scott T. Handy and Mary B. Farone
Antibiotics 2023, 12(9), 1370; https://doi.org/10.3390/antibiotics12091370 - 26 Aug 2023
Viewed by 1071
Abstract
Infections caused by antibiotic-resistant bacteria continue to pose a significant public health threat despite their overall decreasing numbers in the last two decades. One group of compounds fundamental to the search for new agents is low-cost natural products. In this study, we explored [...] Read more.
Infections caused by antibiotic-resistant bacteria continue to pose a significant public health threat despite their overall decreasing numbers in the last two decades. One group of compounds fundamental to the search for new agents is low-cost natural products. In this study, we explored a group of newly synthesized novel aurone-derived triazole compounds to identify those with pharmaceutical potential as inhibitors of antibiotic-resistant Staphylococcus aureus. Using the broth microdilution method, antibacterial activities against methicillin-resistant S. aureus ATCC 43300 (MRSA) and methicillin-sensitive S. aureus ATCC 29213 (MSSA) were identified for four aurone-derived triazole compounds, AT106, AT116, AT125, and AT137, using the half-maximal inhibitory concentrations for the bacteria (IC50) and mammalian cell lines (CC50). Compounds AT125 and AT137 were identified to have pharmaceutical potential as the IC50 values against MRSA were 5.412 µM and 3.870 µM, whereas the CC50 values measured on HepG2 cells were 50.57 µM and 39.81 µM, respectively, resulting in selectivity indexes (SI) > 10. Compounds AT106 and AT116 were also selected for further study. IC50 values for these compounds were 5.439 µM and 3.178 µM, and the CC50 values were 60.33 µM and 50.87 µM, respectively; however, SI values > 10 were for MSSA only. Furthermore, none of the selected compounds showed significant hemolytic activity for human erythrocytes. We also tested the four compounds against S. aureus biofilms. Although AT116 and AT125 successfully disrupted MSSA biofilms, there was no measurable potency against MRSA biofilms. Checkerboard antibiotic assays to identify inhibitory mechanisms for these compounds indicated activity against bacterial cell membranes and cell walls, supporting the pharmaceutical potential for aurone-derived triazoles against antibiotic-resistant bacteria. Examining structure–activity relationships between the four compounds in this study and other aurone-derived triazoles in our library suggest that substitution with a halogen on either the salicyl ring or triazole aryl group along with triazoles having nitrile groups improves anti-Staphylococcal activity with the location of the functionality being very important. Full article
(This article belongs to the Special Issue New Insights into Antimicrobial Compounds: From Synthesis and Discovery to Mechanisms of Action)
►▼ Show Figures

Figure 1

Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-1
Back to TopTop