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Antibiotics
Special Issues
Discovery and Design of New Antimicrobial Agents
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Discovery and Design of New Antimicrobial Agents

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Novel Antimicrobial Agents".

Deadline for manuscript submissions: 5 August 2025 | Viewed by 5658

Special Issue Editor

Dr. Jean Michel Brunel

E-Mail Website
Guest Editor
UMR_MD1, Faculté de Pharmacie, Aix-Marseille Universite, 27 Bd Jean Moulin, CEDEX 5, 13385 Marseille, France
Interests: antimicrobial agents; antibiotic enhancers; organic chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The abuse of antibiotics has accelerated the phenomenon of antibiotic resistance and the discovery of new antimicrobials, as well as the expansion of utility of existing antibiotics, remains a priority to fight the ever-increasing antimicrobial resistance of “superbugs”, pathogenic fungi, etc. This Special Issue of Antibiotics entitled “Discovery and Design of New Antimicrobial Agents” will discuss the chemistry involved in the design and synthesis of original scaffolds, as well as biologically inspired molecules from nature. The structure–activity relationships of these molecules will be also examined to demonstrate the wide interest of chemists as well as biologists, marine scientists, and pharmacologists. The report of strategies to fight antimicrobial resistance by depicting original mechanisms of action against bacteria will be highlighted in this dedicated Special Issue.

Dr. Jean Michel Brunel
Guest Editor

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. 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 agents
  • fight resistance
  • new design
  • structure–activity relationships (SAR)

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (3 papers)

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Research

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17 pages, 8873 KiB  
Article
Isatin Bis-Imidathiazole Hybrids Identified as FtsZ Inhibitors with On-Target Activity Against Staphylococcus aureus
by Rita Morigi, Daniele Esposito, Matteo Calvaresi, Tainah Dorina Marforio, Giovanna Angela Gentilomi, Francesca Bonvicini and Alessandra Locatelli
Antibiotics 2024, 13(10), 992; https://doi.org/10.3390/antibiotics13100992 - 19 Oct 2024
Viewed by 1382
Abstract
In the present study, a series of isatin bis-imidathiazole hybrids was designed and synthesized to develop a new class of heterocyclic compounds with improved antimicrobial activity against pathogens responsible for hospital- and community-acquired infections. A remarkable inhibitory activity against Staphylococcus aureus was demonstrated [...] Read more.
In the present study, a series of isatin bis-imidathiazole hybrids was designed and synthesized to develop a new class of heterocyclic compounds with improved antimicrobial activity against pathogens responsible for hospital- and community-acquired infections. A remarkable inhibitory activity against Staphylococcus aureus was demonstrated for a subset of compounds (range: 13.8–90.1 µM) in the absence of toxicity towards epithelial cells and human red blood cells. The best performing derivative was further investigated to measure its anti-biofilm potential and its effectiveness against methicillin-resistant Staphylococcus aureus strains. A structure–activity relationship study of the synthesized molecules led to the recognition of some important structural requirements for the observed antibacterial activity. Molecular docking followed by molecular dynamics (MD) simulations identified the binding site of the active compound FtsZ, a key protein in bacterial cell division, and the mechanism of action, i.e., the inhibition of its polymerization. The overall results may pave the way for a further rational development of isatin hybrids as FtsZ inhibitors, with a broader spectrum of activity against human pathogens and higher potency. Full article
(This article belongs to the Special Issue Discovery and Design of New Antimicrobial Agents)
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17 pages, 2774 KiB  
Article
Impact of Growth Conditions on High-Throughput Identification of Repurposing Drugs for Pseudomonas aeruginosa Cystic Fibrosis Lung Infections
by Giovanni Di Bonaventura, Veronica Lupetti and Arianna Pompilio
Antibiotics 2024, 13(7), 642; https://doi.org/10.3390/antibiotics13070642 - 12 Jul 2024
Viewed by 1632
Abstract
Pseudomonas aeruginosa lung infections in cystic fibrosis (CF) patients represent a therapeutic challenge due to antibiotic resistance. Repurposing existing drugs is a promising approach for identifying new antimicrobials. A crucial factor in successful drug repurposing is using assay conditions that mirror the site [...] Read more.
Pseudomonas aeruginosa lung infections in cystic fibrosis (CF) patients represent a therapeutic challenge due to antibiotic resistance. Repurposing existing drugs is a promising approach for identifying new antimicrobials. A crucial factor in successful drug repurposing is using assay conditions that mirror the site of infection. Here, the impact of growth conditions on the anti-P. aeruginosa activity of a library of 3386 compounds was evaluated. To this, after 24 h exposure, the survival rate of CF P. aeruginosa RP73 planktonic cells was assessed spectrophotometrically under “CF-like” (artificial CF sputum, pH 6.8, 5% CO2) and enriched (Tryptone Soya Broth, pH 7.2, and aerobiosis) conditions. Among non-antibiotic compounds (n = 3127), 13.4% were active regardless of growth conditions, although only 3.2% had comparable activity; 4% and 6.2% were more active under CF-like or enriched conditions, respectively. Interestingly, 22.1% and 26.6% were active exclusively under CF-like and enriched conditions, respectively. Notably, 7 and 12 hits caused 100% killing under CF-like and enriched conditions, respectively. Among antibiotics (n = 234), 42.3% were active under both conditions, although only 18.4% showed comparable activity; 9.4% and 14.5% were more active under CF-like and enriched conditions, respectively. Interestingly, 23% and 16.6% were active exclusively under CF-like and enriched conditions, respectively. Sulphonamides showed higher activity under CF-like conditions, whereas tetracyclines, fluoroquinolones, and macrolides were more effective under enriched settings. Our findings indicated that growth conditions significantly affect the anti-P. aeruginosa activity of antibiotics and non-antibiotic drugs. Consequently, repurposing studies and susceptibility tests should be performed under physicochemical conditions that the pathogen tackles at the site of infection. Full article
(This article belongs to the Special Issue Discovery and Design of New Antimicrobial Agents)
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Review

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51 pages, 24336 KiB  
Review
An Insight into Rational Drug Design: The Development of In-House Azole Compounds with Antimicrobial Activity
by Daniel Ungureanu, Ovidiu Oniga, Cristina Moldovan, Ioana Ionuț, Gabriel Marc, Anca Stana, Raluca Pele, Mihaela Duma and Brîndușa Tiperciuc
Antibiotics 2024, 13(8), 763; https://doi.org/10.3390/antibiotics13080763 - 13 Aug 2024
Cited by 2 | Viewed by 1952
Abstract
Antimicrobial resistance poses a major threat to global health as the number of efficient antimicrobials decreases and the number of resistant pathogens rises. Our research group has been actively involved in the design of novel antimicrobial drugs. The blueprints of these compounds were [...] Read more.
Antimicrobial resistance poses a major threat to global health as the number of efficient antimicrobials decreases and the number of resistant pathogens rises. Our research group has been actively involved in the design of novel antimicrobial drugs. The blueprints of these compounds were azolic heterocycles, particularly thiazole. Starting with oxadiazolines, our research group explored, one by one, the other five-membered heterocycles, developing more or less potent compounds. An overview of this research activity conducted by our research group allowed us to observe an evolution in the methodology used (from inhibition zone diameters to minimal inhibitory concentrations and antibiofilm potential determination) correlated with the design of azole compounds based on results obtained from molecular modeling. The purpose of this review is to present the development of in-house azole compounds with antimicrobial activity, designed over the years by this research group from the departments of Pharmaceutical and Therapeutical Chemistry in Cluj-Napoca. Full article
(This article belongs to the Special Issue Discovery and Design of New Antimicrobial Agents)
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