Antimicrobial and Antibiofilm Activity of Auranofin and Its Two Derivatives Bearing Naproxen and Acetylcysteine as Ligands Against Staphylococci

Antibiotics, Год журнала: 2025, Номер 14(2), С. 118 - 118

Опубликована: Янв. 23, 2025

Background/Objectives: The ability of bacteria to form biofilms makes them more tolerant traditional antibiotics. Given the lack new antibiotic development, drug repurposing offers a strategy for discovering treatments. Auranofin (AF), gold-based compound indicated treatment rheumatoid arthritis, shows promising antibacterial activity. This study investigates antimicrobial and antibiofilm activity AF its two derivatives in which thiosugar ligand is replaced by acetylcysteine (AF-AcCys) or naproxen (AF-Napx), against Staphylococcus aureus epidermidis. Methods: was conjugated transmetalation with either acetylcysteine. Assessments their stability DMSO/H2O lipophilicity expressed as LogP were performed. analogues investigated broth microdilution assay determine minimum inhibitory concentration (MIC) versus biofilm obtain bactericidal (MBBC) eradication (MBEC). Results: found be stable mixture 48 h. AF-Napx showed = 1.25 ± 0.22, close AF, while AF-AcCys had −0.95. MIC values S. epidermidis ranging from 2 µM 0.25 µM, ≤0.12 respectively. Both maintained efficacy biofilm-embedded at non-cytotoxic concentrations, demonstrating lower MBBC Conclusions: especially conjugate, holds potential therapeutic agent treating biofilm-associated infections caused epidermidis, particularly device-related where both infection inflammation are present.

Язык: Английский

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Curcumin-derived water-soluble carbon dots without detectable resistance: Dual potentials for antimicrobial activity and infected wound healing

Diamond and Related Materials, Год журнала: 2025, Номер 153, С. 112075 - 112075

Опубликована: Фев. 6, 2025

Язык: Английский

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Superior antibacterial activity of Cu-Ag co-doped nano-ZnO synthesized by one-step method

Materials Today Communications, Год журнала: 2025, Номер unknown, С. 112520 - 112520

Опубликована: Апрель 1, 2025

Язык: Английский

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An organometallic hybrid antibiotic of metronidazole with a Gold(I) N-Heterocyclic Carbene overcomes metronidazole resistance in Clostridioides difficile

JBIC Journal of Biological Inorganic Chemistry, Год журнала: 2024, Номер 29(5), С. 511 - 518

Опубликована: Июнь 26, 2024

Antimicrobial resistance (AMR) has been emerging as a major global health threat and calls for the development of novel drug candidates. Metal complexes have demonstrating high efficiency antibacterial agents that differ substantially from established types antibiotics in their chemical structures mechanism action. One strategy to exploit this potential is design metal-based hybrid organometallics consist an antibiotic warhead contributes additional action different parent antibiotic. In communication, we describe organometallic 2c, which metronidazole connected gold(I) N-heterocyclic carbene inhibits bacterial thioredoxin reductase (TrxR). Metronidazole can be used treatment with obligatory anaerobic pathogen Clostridioides difficile (C. difficile), however, hampers its clinical success. The gold conjugate 2c was efficient inhibitor TrxR it inactive or showed only minor effects against eucaryotic cells bacteria grown under aerobic conditions. contrast, strong effect observed both metronidazole-sensitive -resistant strains C. difficile. This report presents proof-of-concept viable approach efficiently tackle AMR.

Язык: Английский

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Attaching Metal-Containing Moieties to β-Lactam Antibiotics: The Case of Penicillin and Cephalosporin

Inorganic Chemistry, Год журнала: 2024, Номер 63(27), С. 12593 - 12603

Опубликована: Июнь 26, 2024

Procedures for the preparation of transition metal complexes having intact bicyclic cepham or penam systems as ligands have been developed. Starting from readily available 4-azido-2-azetidinones, a synthetic approach has tuned using copper-catalyzed azide–alkyne cycloaddition between 3-azido-2-azetinones and alkynes, followed by methylation transmetalation to Au(I) Ir(III) mesoionic carbene Ag(I) complexes. This methodology was applied 6-azido 7-azido derivatives build 6-(1,2,3-triazolyl)penam 7-(1,2,3-triazolyl)cepham proligands, which upon metalation with yielded products derived coordination C6 C7 positions, preserving structure penicillin cephalosporin scaffolds. The crystal complex 28b, an Ir atom directly bonded bicycle, determined X-ray diffraction. is first structural report penicillin-transition-metal system these antibiotics intact. selectivity processes interpreted DFT calculations.

Язык: Английский

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Liposomal Formulation of a Gold(III) Metalloantibiotic: A Promising Strategy Against Antimicrobial Resistance.

Dalton Transactions, Год журнала: 2024, Номер 53(36), С. 15205 - 15214

Опубликована: Янв. 1, 2024

A novel lipoformulation was developed by encapsulating cationic (S^C)-cyclometallated gold(III) complex [Au(dppta)(N

Язык: Английский

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In the search for new gold metalloantibiotics: In vitro evaluation of Au(III) (C^S)-cyclometallated complexes

Journal of Inorganic Biochemistry, Год журнала: 2024, Номер 262, С. 112735 - 112735

Опубликована: Сен. 10, 2024

Язык: Английский

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Regulating Energy Transfer Pathways to Construct Multicolor Luminescent Lanthanide Metal–Organic Frameworks and Their Multiorder Anticounterfeiting Barcodes and Antibiotic Sensing

ACS Materials Letters, Год журнала: 2024, Номер unknown, С. 4911 - 4921

Опубликована: Окт. 2, 2024

Язык: Английский

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Synthesis, structural determination, and antibacterial studies of Silver(I) and Gold(I) benzimidazolylidene complexes with N-tert-butylacetyl fragments

Journal of Molecular Structure, Год журнала: 2024, Номер unknown, С. 140822 - 140822

Опубликована: Ноя. 1, 2024

Язык: Английский

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Xylose Incorporated in Unsymmetrical Gold(I) N‐Heterocyclic Carbene Complexes: Synthesis, Characterization and Antibacterial Activity

ChemMedChem, Год журнала: 2024, Номер 19(22)

Опубликована: Авг. 1, 2024

Abstract A series of Au(I) complexes containing unsymmetrical N ‐heterocyclic carbene (imidazolylidene and benzimidazolylidene) functionalized with a xyloside group an alkyl moiety (methyl mesityl) was prepared using efficient procedures from D‐xylose. Their characterization carried out in solution by multinuclear NMR, HR‐MS spectrometry cyclic voltammetry, as well the solid state means single crystal X‐ray diffraction analysis for two them. Evaluation their ability to inhibit bacterial growth showed preference Gram‐positive strain, Staphylococcus aureus , over Gram‐negative Pseudomonas aeruginosa .

Язык: Английский

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