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Antibiotics
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Antibiotic Synthesis, 2nd Edition
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Antibiotic Synthesis, 2nd Edition

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

Deadline for manuscript submissions: 31 October 2026 | Viewed by 3437

Special Issue Editors

Prof. Dr. Naresh Kumar

E-Mail Website
Guest Editor
School of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia
Interests: biologically active molecules; medicinal chemistry; organic chemical synthesis; peptidomimetics; novel antimicrobials; biomaterials
Special Issues, Collections and Topics in MDPI journals
Dr. Tsz Tin Yu

E-Mail Website
Guest Editor
School of Chemistry, University of New South Wales (UNSW Sydney), Sydney, NSW 2052, Australia
Interests: medicinal chemistry; antimicrobials; peptidomimetics; quorum sensing; Antibiofilm
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The emergence of multidrug-resistant bacteria threatens the effectiveness of current antibiotics. It is projected that by 2050, antimicrobial resistance will cause 10 million deaths annually. Bacteria continue to evolve at a rate that surpasses drug development, highlighting a necessity for new drugs with mechanisms that inhibit resistance development. Furthermore, this situation is exacerbated by a reduction in the pace of development of novel classes of antibiotics.

Potential strategies to overcome this dilemma are highlighted below:

i) Discovery of new antimicrobial agents from natural sources and their synthetic derivatives;
ii) The design and synthesis of antimicrobial compounds with novel mechanisms of action;
iii)  Targeted delivery of antimicrobial agents;
iv) Combination therapy involving antibiotics and new antimicrobial agents;
v) Synthesis of dual- and multi-action antibiotics;
vi) Synthesis of adjuvants to enhance the potency of antibiotics;
vii) Exploiting innate bacterial responses to develop new antibiotics.

The Special Issue will publish contemporary research on the discovery and development of new classes of antibiotic compounds, as well as dual-action antimicrobials and other combination strategies. It is my pleasure to invite submissions of high-quality research-based papers related to the topics mentioned above.

Prof. Dr. Naresh Kumar
Dr. Tsz Tin Yu
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 250 words) can be sent to the Editorial Office for assessment.

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

  • new antimicrobial compounds
  • dual-action antimicrobials
  • new antimicrobial targets
  • targeted delivery of antibiotics
  • new scaffolds for antimicrobial discovery
  • discovery of new antimicrobial mechanisms

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Published Papers (3 papers)

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Research

38 pages, 3263 KB  
Article
Thiazolyl-Methylthio-1,3,4-Thiadiazole Hybrids as Halicin Analogues with Antimicrobial and Antibiofilm Activities: Chemical Development, Biological Assessment, and 2D-QSAR Study
by Daniel Ungureanu, Gabriel Marc, Mihaela Niculina Duma, Dan Cristian Vodnar, Gheorghe-Adrian Martău, Laurian Vlase, Adrian Pîrnău, Brîndușa Tiperciuc, Cristina Moldovan, Ioana Ionuț, Anca Stana, Ilioara Oniga and Ovidiu Oniga
Antibiotics 2026, 15(5), 448; https://doi.org/10.3390/antibiotics15050448 - 29 Apr 2026
Viewed by 425
Abstract
Background/Objectives: The purpose of this study was the chemical design, synthesis, and evaluation of the antimicrobial and antibiofilm potentials of 20 novel thiazolyl-methylthio-thiadiazole hybrid compounds (6a–j and 8a–j). Methods: The compounds were designed as structural [...] Read more.
Background/Objectives: The purpose of this study was the chemical design, synthesis, and evaluation of the antimicrobial and antibiofilm potentials of 20 novel thiazolyl-methylthio-thiadiazole hybrid compounds (6a–j and 8a–j). Methods: The compounds were designed as structural analogues of halicin with two points of variation and were synthesized through a process with multiple condensation steps. The compounds were evaluated in vitro through MIC determinations for the antimicrobial activity and percentage of biofilm inhibition, and in silico, respectively, through molecular docking, druggability, and ADMETox prediction. A 2D-QSAR study was conducted for antimicrobial activity using the Free-Wilson model. Results: In terms of antibacterial activity, all compounds displayed important activity on the tested strains (MICs = 15.62–250 μg/mL), except against Staphylococcus aureus. Regarding the antifungal activity, the effect against Candida albicans was similar to fluconazole in most cases (MIC = 15.62 μg/mL). With respect to the antibiofilm activity, the most effective activity was registered against the Pseudomonas aeruginosa biofilm. The in vitro results for the antibacterial activity against Escherichia coli were correlated with the observations drawn in the molecular docking study on the ATPase domain of the GyrB subunit of E. coli. The in silico predictions of the molecular properties concluded that all compounds have good druggability properties, while the ADMETox predictions concluded that the compounds could have low gastrointestinal absorption and blood–brain barrier permeation capacity, but raised safety flags (e.g., hepatotoxicity and high acute oral toxicity). The 2D-QSAR study concluded that the thiazolyl-methylthio-thiadiazole scaffold had the highest contribution to antimicrobial activity in almost all cases. Conclusions: The two series of compounds highlight the impact of structural modulations of the scaffold and its substituents on the investigated biological activities. Full article
(This article belongs to the Special Issue Antibiotic Synthesis, 2nd Edition)
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17 pages, 2458 KB  
Article
Impact of the Transcriptional Regulator SCO7424 Overexpression on Antibiotic Production in Streptomyces coelicolor
by Gladys Vega-Sauceda, Karen Villarreal-Gómez, Beatriz Ruiz-Villafán, Romina Rodríguez-Sanoja and Sergio Sánchez
Antibiotics 2026, 15(1), 70; https://doi.org/10.3390/antibiotics15010070 - 8 Jan 2026
Viewed by 899
Abstract
Background. The genus Streptomyces is known for its capability to produce a wide range of bioactive secondary metabolites. The enzymes required for their synthesis are encoded within biosynthetic gene clusters (BGCs), whose expression can be influenced by various physical and nutritional factors. Among [...] Read more.
Background. The genus Streptomyces is known for its capability to produce a wide range of bioactive secondary metabolites. The enzymes required for their synthesis are encoded within biosynthetic gene clusters (BGCs), whose expression can be influenced by various physical and nutritional factors. Among these nutritional factors, it is worth highlighting carbon catabolic repression (CCR), which prevents the formation of secondary metabolites. It has been shown that transcriptional factors, in turn, regulated by glucose or by the enzyme glucose kinase (Glk), may be involved in this mechanism. It was shown that the expression of some transcriptional factors is regulated by glucose availability and that the enzyme glucose kinase (Glk) may play a role in this process. One of the transcriptional factors most upregulated in the presence of glucose/agar in Streptomyces coelicolor M145 is SCO7424, a member of the MarR family of transcriptional regulators. However, its influence on antibiotic synthesis has never been studied. Objective. In this work, we evaluated the effect of SCO7424 overexpression on the synthesis of actinorhodin (ACT) and undecylprodigiosin (RED), and its impact on growth and glucose consumption. Methods. A copy of the sco7424 gene was cloned into the pIJ702 plasmid, which was then transformed into a wild-type strain of S. coelicolor M145. Growth and antibiotic production were evaluated in the strain with two copies of sco7424 and in the wild-type strain. We also evaluated the expression of the probable target genes by quantitative RT-PCR. Results. We found that overexpression of sco7424 negatively impacts growth, glucose consumption kinetics, and the expression of specific regulators of the ACT and RED biosynthetic pathways, resulting in reduced ACT and RED production. Understanding the function of the regulatory cascades regulated by this family of regulators is crucial for boosting the yields of valuable metabolites produced by industrial strains. Full article
(This article belongs to the Special Issue Antibiotic Synthesis, 2nd Edition)
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29 pages, 5042 KB  
Article
Tuning the Structure–Functional Properties Within Peptide-Mimicking Antimicrobial Hydrogels
by Samuel T. Attard, Vina R. Aldilla, Rajesh Kuppusamy, Renxun Chen, David StC Black, Pall Thordarson, Mark D. P. Willcox and Naresh Kumar
Antibiotics 2025, 14(11), 1118; https://doi.org/10.3390/antibiotics14111118 - 5 Nov 2025
Cited by 1 | Viewed by 1565
Abstract
Background/Objectives: There is a growing demand for the development of novel antimicrobial agents due to their efficacy being eroded by increasing antimicrobial resistance. Antimicrobial hydrogels have been reported as a method to treat bacterial infections. Methods: This study explores how different structural features [...] Read more.
Background/Objectives: There is a growing demand for the development of novel antimicrobial agents due to their efficacy being eroded by increasing antimicrobial resistance. Antimicrobial hydrogels have been reported as a method to treat bacterial infections. Methods: This study explores how different structural features are important for the hydrogelation properties of amphiphilic antimicrobial peptide-mimics through rheology and AFM, as well as properties important for antimicrobial activity measured through MIC. Results: Eleven novel peptide-mimicking anthranilamides containing various structural features were synthesised in 4–7 steps. Of these peptide-mimics, three novel compounds formed hydrogels, and it was identified that their mechanical strength, secondary structure, and fibre morphology could be tuned by altering the aromatic cap or the amino acid side chain. In conjunction, several structural features were identified that reduce hydrogelation strength and stiffness. Conclusions: This work provides an insight into how the structural features of low-molecular-weight self-assembling hydrogels can translate to differing physical and potent antimicrobial properties. This work provides a rational guide to optimising physical hydrogel properties, as well as highlighting features that may reduce hydrogelation. Full article
(This article belongs to the Special Issue Antibiotic Synthesis, 2nd Edition)
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