Antibiotics

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Dr. Nikoletta Szemerédi

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Department of Medical Microbiology, Albert Szent-Györgyi Health Center and Albert Szent-Györgyi Medical School, University of Szeged, Semmelweis u. 6, H-6725 Szeged, Hungary
Interests: antibiotic resistance; biofilm; efflux pumps

Dr. Diana I.S.P. Resende

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1. LQOF—Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge de Viterbo Ferreira 228, 4050-313 Porto, Portugal
2. CIIMAR/CIMAR LA—Centro Interdisciplinar de Investigação Marinha e Ambiental, Universidade do Porto, Terminal de Cruzeiros do Porto de Leixões, 4450-208 Matosinhos, Portugal
3. ICBAS—Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto, Rua de Jorge de Viterbo Ferreira 228, 4050-313 Porto, Portugal
Interests: organic chemistry; synthesis; natural products
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Special Issue Information

Dear Colleagues,

The rise in antimicrobial resistance poses a critical global health threat, necessitating the development of novel therapeutic agents capable of overcoming resistant pathogens. This Special Issue in Antibiotics focuses on the design, synthesis and biological evaluation of innovative antimicrobial compounds targeting resistance mechanisms. Emphasis is placed on rational drug design strategies that exploit molecular insights into bacterial resistance, including efflux pump inhibition, enzymatic degradation avoidance, quorum sensing inhibition and disruption of biofilm formation. Contributions may encompass the synthesis of molecules, peptides, or hybrid scaffolds, alongside structure-activity relationship studies and mechanistic investigations. Biological evaluation includes in vitro and in vivo assessments of antimicrobial efficacy, cytotoxicity and resistance-modulating potential. By integrating chemistry, microbiology and pharmacology, this issue aims to showcase cutting-edge approaches to combat multidrug-resistant infections, providing a platform for novel agents that could reinvigorate the antibiotic pipeline and inform future clinical development. Interdisciplinary research addressing both molecular innovation and translational relevance is particularly encouraged.

Dr. Nikoletta Szemerédi
Dr. Diana I.S.P. Resende
Guest Editors

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16 pages, 842 KB

Open AccessArticle

Synthesis of α-Santonin Derivatives Linked to N-, S-, and O-Heterocycles via 1,2,3-Triazole-Linker: Investigation of Antimicrobial Effects

by Mária Fanni Boncz, Kitti Tari, András Szekeres, Adriána Kovács, István Zupkó, Tam Minh Le and Zsolt Szakonyi

Antibiotics 2026, 15(6), 611; https://doi.org/10.3390/antibiotics15060611 - 16 Jun 2026

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Abstract

Background/Objectives: Resistant pathogenic bacteria and fungi are a growing problem worldwide; therefore, the discovery of new active ingredients is an important challenge for which the functionalization of natural terpenes with biologically active heterocycles can provide a basis. To reach this goal, a series of 1,4-disubstituted-1,2,3-triazole conjugates was designed and synthesized starting from commercially available α-santonin. Methods: The key azido derivative intermediate was prepared according to literature procedures via Michael addition between dehydrosantonin and the TMSN₃/AcOH/Et₃N system at its highly reactive α-methylene-γ-lactone motif. Subsequently, the obtained azide was applied to regioselective Huisgen 1,3-dipolar cycloaddition reaction with a wide range of terminal alkynes bearing N-, S- and O-heterocycles. These include pyridine, pyrimidine, purine, quinoline, indol, or coumarin to afford the sesquiterpene–heterocycle chimaeras. All triazole conjugates were screened for in vitro antiproliferative activity by MTT assay against HeLa, MDA-MB231, SiHa, MCF-7 and A2780 human cancer cell lines compared with fibroblast cells (NIH/3T3) to check their cytotoxicity and antimicrobial effects on two Gram-positive (B. subtilis, S. aureus) pathogenic bacteria, two Gram-negative (E. coli and P. aeruginosa) pathogenic bacteria, and two yeasts (C. krusei and C. albicans). Results: The results indicated that most of the examined compounds expressed weak activity against human cell lines, while some of them showed moderate activity against S. aureus (up to 99% inhibition at 100 µg/mL conc.), C. krusei (up to 51% inhibition at 10 µg/mL conc.) and C. albicans (up to 52% inhibition at 10 µg/mL conc.). Conclusions: Further structural modification of the best, selective antibacterial and antifungal compounds may open the possibility to the development of effective natural sesquiterpene-based selective antimicrobial agents. Full article

(This article belongs to the Special Issue Design, Synthesis, and Biological Evaluation of Novel Antimicrobial Agents Targeting Resistance Mechanisms)

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