Antibacterial Research Articles

Novel antibacterial pullulan derivatives modified with quaternary phosphonium salts for infected wound treatments

The development of novel antibacterial agents is urgently needed to tackle bacterial infection, the major global issue menacing human health. Among them, polymeric quaternary phosphonium salts are worth noticing owing to their strong antibacterial activities and other merits including low bacterial drug resistance. Herein, pullulan modified with quaternary phosphonium salts (PQP) was synthesized using esterification reactions of pullulan and (5-carboxypentyl)triphenylphosphonium bromide (CPTPPB) mediated by N,N′‑carbonyldiimidazole (CDI), and was evaluated as novel antibacterial agents for treating wound infection for the first time. The chemical structures, chemical bonding, elemental compositions, crystalline properties and thermostability of PQP were systematically investigated. PQP exhibited in vitro antibacterial activities against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli), which were unveiled by the spread plate method and possibly resulted from the damage of bacterial cell walls/membranes mediated by electrostatic and hydrophobic interactions according to preliminary mechanism studies. Weak cytotoxicity and excellent hemocompatibility of PQP at the effective bactericidal concentration were observed. Moreover, in the infected wound model of mice, PQP was capable of disinfecting the wound and accelerating the healing. We opine PQP in this work is promising for antibacterial applications and will inspire the synthesis of novel antibacterial agents derived from natural polymers.

Effectiveness of rifampicin combination therapy for orthopedic implant-related infections: A systematic review and meta-analysis

BackgroundIn vitro, animal, and clinical comparative studies have revealed that combinations of rifampicin with antibacterial agents are effective in the treatment of biofilm-associated infections. This study aimed to assess the effectiveness of rifampicin combination therapies compared with monotherapies without rifampicin in patients with orthopedic implant-related infections. Materials and MethodsThe clinical literature was comprehensively searched for studies assessing the effectiveness of rifampicin combination therapy in patients with orthopedic implant-related infection. Identified studies were screened based on the PRISMA flow diagram. The primary outcome was the cure rate and the secondary outcome was the incidence of adverse events. Subgroup analyses were performed based on causative organisms, antibacterial agents, and types of surgical intervention. ResultsTwenty-seven studies were identified, including two randomized controlled trials (RCTs) and 25 cohort studies. Rifampicin combinations were associated with significantly higher cure rates than monotherapies in cohort studies, but not in RCTs. Subgroup analyses showed that rifampicin combinations were effective in patients infected with Cutibacterium and Staphylococcus spp.; in patients who underwent debridement, antibiotics, implant retention (DAIR) procedures; and in patients with one-stage revision. Moreover, combinations of rifampicin and fluoroqinolones were more effective than fluoroquinolones alone, while combinating rifampicin with other antibacterial agents showed no significant benefit. Combination treatment did not significantly affect adverse events in either RCTs or observational studies. Risk of bias assessment and summary of findings showed that the certainty of evidence for both RCTs and observational studies was very low. ConclusionThis systematic review and meta-analysis confirmed the potential effectiveness of rifampicin combination therapy for the cure of orthopedic implant-related infection in some circumstances, although the certainty and quality of evidence were very low.

New Schiff Base Derived Organotin (IV) Complexes: Synthesis, Characterization, In vitro and In silico Biological Studies

Aims: The creation and testing of new Schiff base-based antibacterial organotin (IV) complexes were the objectives of this investigation. Background: Due to developed resistance, antibiotics that were once often used to treat microor-ganisms are no longer effective against them. It is thought that organotin compounds synthesized from Schiff bases have significant pharmacological effectiveness and work well as antibacterial agents. Methods: Thiocarbohydrazide and dehydroacetic acid were condensed to create the Schiff base, followed by processing with dialkyltin(IV)dichloride to synthesize the final product. Modern an-alytical techniques were used to clarify the compounds' probable structural details. The crystalline nature of the produced compounds was tested using PXRD. Results: All of the compounds were thermally stable up to 300°C. All of the synthesized com-plexes showed potent antibacterial activity in the range of 250 to 400 μg/ml. Furthermore, the computational biology research showed that, in contrast to ligands, which had a binding energy of -7.3 to -7.4 kcal/mol, complexes interacted well with dihydropteroate synthase and DNA gy-rase. Conclusion: The current study offered a unique technique for synthesizing diorganotin(IV) de-rivatives of N-substituted Schiff bases that are physiologically active. The results show that the chemicals created are promising antibacterial mediators against diseases that affect humans in the modern world. It might also open the door to future studies on drug-resistant microorganisms that could have biological uses.

CdO Nanoparticles by chemical method as antimicrobial therapy in order to maintain of healthy cells

Abstract A simple chemical method that has the potential for large-scale manufacturing was used to produce Cadmium Oxide (CdO) Nanoparticles (NPs). Using X-ray diffraction (XRD), atomic force microscopy (AFM), Fourier transform infrared (FTIR), and ultraviolet-visible (UV-vis) spectroscopy, The optical and Structural properties of synthesized CdO were investigated, strong antibacterial activity of CdO nanoparticles is demonstrated against a variety of Gram-positive, Gram-negative, and fungal diseases. Therefore, CdO NPs might be a potential substitute to develop as an antibacterial agent against bacterial strains that are resistant to many drugs. Applications of CdO NPs might provide important discoveries in a variety of domains, including antibacterial systems and medical devices.

Double-crosslinked polyvinyl alcohol/starch bioplastic with superior water-resistance and flame retardancy

The high water solubility and flammability of polyvinyl alcohol (PVA) limits its further widespread use in areas such as bioplastic and green packaging. In this study, double-crosslinked polyvinyl alcohol/starch bioplastics (named PDA) were fabricated using PVA, dialdehyde starch (DAS), and phytic acid (PA), resulting in a material with superior water resistance, flame retardancy, and excellent degradability. PA not only plays the role of catalyst for the chemical crosslinking but also as the physical crosslinker to form the intermolecular hydrogen bonds with PVA and DAS. This chemically and physically double cross-linked network structure results in PDA bioplastics with excellent toughness and water resistance. Specifically, the optimal formulation with 15 % PA content, designated as PDA15, exhibited a high toughness of 35.5 MJ/m3 and demonstrated prolonged shape retention in the boiling water. Additionally, PA also serves as a flame-retardant and antibacterial agent; the PDA15 achieved a high limit oxygen index (LOI) value of 40.0 % and passed the UL-94 V-0 rating without melt dripping, along with better degradability compared to pure PVA film. These outstanding performances make the PDA bioplastics highly promising for various applications, particularly in disposable plastics and laminated flexible packaging materials.

Synthesis of new 1,4-benzodioxin derivatives containing thiazolidin-4-one skeleton, molecular modelling and docking as antibacterial agents

In this study, we synthesized a variety of 1,4-benzodioxin derivatives containing the thiazolidin-4-one skeleton and evaluated their antimicrobial properties. Several of the newly synthesized compounds exhibited potent inhibitory effects against the Gram-negative bacteria Escherichia coli. By conducting molecular docking simulations and molecular dynamics with the fatty acid synthesis enzyme FabH, we unveiled the potential antimicrobial activity of these compounds, suggesting they interfered with fatty acid biosynthesis pathways. Additionally, we optimized compound 3b and assessed its ability to disrupt biofilms using live/dead cell staining techniques. The results highlighted significant biofilm disruption, enhancing the compounds' antimicrobial efficacy. These findings provided valuable insights for the development of novel antimicrobial agents and presented a promising avenue for addressing antimicrobial resistance through innovative therapeutic approaches.

Insights into Antibacterial Design: Computational Modeling of Eugenol Derivatives Targeting DNA Gyrase

The rise of antibiotic resistance underscores the urgent need for novel antibacterial agents. DNA gyrase, an essential enzyme involved in bacterial DNA replication, is a promising target for antibacterial therapy. Computational approaches offer a cost-effective means to design and screen potential inhibitors, such as eugenol derivatives. This study aims to computationally design eugenol derivatives as potential antibacterial agents targeting DNA gyrase, assess their binding affinities, evaluate physicochemical properties, and toxicity, and select lead compounds for further investigation. Molecular docking simulations were conducted to investigate the binding affinities of eugenol derivatives and controls to DNA gyrase. Physicochemical properties and toxicity assessments of eugenol were evaluated. Lead compounds were selected based on drug likeness, toxicity, and binding affinity. Molecular docking studies revealed varying binding affinities of eugenol derivatives to DNA gyrase, with lead compounds exhibiting superior affinity compared to eugenol. Physicochemical properties indicated moderate lipophilicity and low aqueous solubility for eugenol. Toxicity assessment revealed mutagenicity and tumorigenicity. De novo compound synthesis generated 244 novel compounds, with 44 selected based on drug-likeness, toxicity, and binding affinity as lead candidates. These findings provide valuable insights for the development of novel antibacterial agents targeting DNA gyrase, with implications for combating antibiotic resistance.

Locust bean gum-based silver nanocomposite hydrogel as a drug delivery system and an antibacterial agent.

Effective drug release is of utmost importance in the medical field for treating various diseases, particularly cancer. Nanocomposite hydrogels remain the best materials for enhancing the bioavailability and therapeutic levels of drugs as they enable sustained, targeted, or controlled drug release. In this work, a nanocomposite hydrogel containing locust bean gum (LBG), poly(4-acryloylmorpholine) (PAcM), and silver nanoparticles (SN) has been made using an eco-friendly microwave (MW)-assisted method and characterized by various advanced techniques. The material is evaluated for its potential as a matrix material towards delivering 5-fluorouracil (5-FU), an anticancer drug in the gastrointestinal tract, and inhibiting bacterial growth. The pH-dependency of the nanocomposite materials towards swelling and drug release and its antibacterial characteristics have been compared with the neat gel in order to understand the role of SN in enhancing the performance of the materials. The results indicated both polymer materials exhibit a pH-dependent release of 5-FU with a higher release at pH 1.2, simulated gastric fluid, than at pH 7.4, simulated intestinal fluid. About 72 % of the loaded drug was released from the nanocomposite, as compared to 44 % from neat gel at pH 1.2 during the observation period of 3 h. The drug release process could be best explained by the first-order kinetic model and Fickian diffusion transport mechanism. The nanocomposite exhibited remarkable antibacterial activity against Staphylococcus aureus and Escherichia coli. The biocompatibility of the drug-loaded nanocomposite was demonstrated by a cytotoxicity study, which showed higher than 80 % viability of healthy IEC-6 cells. The results indicate the suitability of the developed nanocomposite material as a polymer matrix for sustained release of 5-FU in cancer therapy and also as an antibacterial agent to fight against bacterial infections.

Preparation and characterization of porous corn starch-based antibacterial sustained-release intelligent film

A novel porous corn starch-based antibacterial sustained-release intelligent film was prepared with the porous corn starch as the substrate, purple corn cob anthocyanin (PCA) as the indicator, and tangerine peel essential oil as the antibacterial agent, and its properties were studied. The results showed that the porous corn starch-based antimicrobial sustained-release indicator film had good mechanical strength, surface hydrophobicity and light transmittance. The tensile strength of the sustained-release indicator film (PLSt-12) prepared by porous corn starch with an enzymatic hydrolysis time of 12 h was 14.35 MPa and the elongation at break was 6.55 %. The water contact angle was 89.10°, and the water vapor transmittance was 6.62 × 10−4 g·mm2·s−1·Pa−1. The PLSt-12 was brown at pH 10 and had a sensitive color response. The PLSt-12 reduced the release rate of anthocyanins by 25.01 %, and the sustained-release mechanism was non-Fick diffusion. It showed a significant color change when the pork quality deteriorated, which can be used to monitor the freshness of the pork. This type of antibacterial sustained-release intelligent film had considerable application potential in indicating food freshness.

Synthesis of new pyrazoles, thiadiazoles, and trizolotriazines compounds that act as an antibacterial agents using C-ethoxycarbonylhydrazonoyl chloride precursor: Molecular docking simulation and in silico ADMET prediction studies

Treatment of C-ethoxycarbonylhydrazonoyl chloride with active methylene-containing compounds such as dibenzoylmethane or malononitrile in sodium ethoxide solution yielded in each case pyrazole derivatives. The latter pyrazoles were used as a useful precursors in the synthesis of new heterocyclic compounds like pyrazoles and 1,3,4-thiadizaoles upon reaction with hydrazonoyl halides. Also, the reaction of C-ethoxycarbonylhydrazonoyl chloride with the approperiate triazinethiones in chloroform in the presence of catalytic amount of triethylamine at reflux yielded the corresponding triazolotriazines. The structures of the newly synthesized compounds were confirmed based on elemental analyses and spectral data. The antibacterial activities were studied against two gram-positive and two gram-negative bacteria, the results represented that compound 26a showed antibacterial activity against Salmonella (22 mm) and E. coli (6 mm), as well as compound 26b against Salmonella (5 mm) and Staphylococcus aureus (10 mm) while the rest compounds showed no antibacterial activities. The molecular docking simulation was investigated for the most active compounds 26a and 26b. The results confirm that compounds 26a and 26b are promising candidates for potential inhibitors of DNA gryA (P37411) of Salmonella and Transpeptidases of Staphylococcus aureus.

In Silico ADME And Molecular Docking Studies of New Thiazolyl-bipyrazole, Pyrazolopyridine and Pyrano[2,3-d]pyrazolopyridine Derivatives as Antibacterial Agents

: In this study, a series of novel pyrazole-based compounds were synthesized starting from the precursor ethyl 3-(4-amino-1-phenyl-3-((4-sulfamoylphenyl)carbamoyl)-1Hpyrazol- 5-yl)-3-oxopropanoate (2). Various synthetic routes were used to obtain pyrazolylpyrazolone 3, tricyclic dipyrazolopyridine 4a-c, thiazolyl-bipyrazoles 5 & 6, pyrazolo[4,3- b]pyridines 7 & 9, and tricyclic pyranopyrazolopyridine 10a–c. These compounds were screened for their antibacterial activity against four bacterial strains. The promising candidates 4a, 4b, 4c, 7, 9, and 10c exhibited minimum inhibitory concentrations ranging from 0.98 to 31.25 μg/mL. The in silico ADME properties for the active compounds exhibited similar physiochemical properties, with compound 9 demonstrating the best likeness and no inhibition effect on the popular drug metabolism enzyme CYP. Molecular docking simulations highlighted compounds 9 and 10c as potent antibacterial agents via DNA-gyrase inhibition

Coral-like AgNPs hybrided MOFs modulated with biopolymer polydopamine for synergistic antibacterial effect and biofilm eradication.

Bacterial contamination is an intractable challenge in food safety, environments and biomedicine fields, and places a heavy burden on society. Polydopamine (PDA), a high molecular biopolymer, is considered as a promising candidate to participate in the design of novel antibacterial agents with unique contributions in biocompatibility, adherence, photothermal and metal coordination ability. In this study, coral-like ZIFL-PDA@AgNPs with excellent antibacterial properties and biocompatibility were prepared by embedding AgNPs into the biopolymer PDA-modulated ZIFL-PDA nanostructures by green reduction method to solve the problem of poor stability of AgNPs. Based on the plasma resonance effect of AgNPs, coral-like ZIFL-PDA@AgNPs had enhanced photothermal properties compared with ZIFL-PDA. Due to the synergistic effect between antibacterial metal ions mainly Ag+ and the photothermal effect, coral-like ZIFL-PDA@AgNPs showed enhanced anti-mature biofilm and antibacterial properties, which was dependent on its concentration and sterilization time. In addition, regulated by the ZIFL-PDA nanostructure, coral-like ZIFL-PDA@AgNPs demonstrated a unique Ag+ long-time sustained release behavior, giving it an extended antibacterial validity period and good biocompatibility. Antibacterial mechanism experiments indicated that coral-like ZIFL-PDA@AgNPs can significantly damage the integrity of bacterial cell membrane, reduce the content of ATP in bacterial by affecting the activity of succinate dehydrogenase, and induce the accumulation of reactive oxygen species, ultimately leading to bacterial death.

One-bath dyeing and antibacterial finishing of cotton fabric using reactive dye and silver chloride: a sustainable approach

One-bath dyeing and antibacterial finishing of cotton fabric using reactive dye as colorant and silver chloride (AgCl) as an antibacterial agent was conducted to streamline the process and enhance its economic efficiency. The effectiveness of the antibacterial agent in reactive dyeing of cotton fabric, was evaluated through exhaust method with 0.5% AgCl and continuous (pad dry cure) method with 5 g/l of AgCl, utilizing various dye concentrations (1%, 3%, 5% for exhaust; 1g/l, 3g/l, 5g/l for pad dry cure) according to a standard reactive dye recipe. Characterization of the one-bath dyed, and antibacterial finished cotton fabric was performed using K/S values to determine the optimal dye shade concentration and antibacterial activity was evaluated using agar diffusion method. It was observed that the exhaust method revealed an optimum dye concentration at (AgCl 0.5% and dye 5%), while pad dry cure method showedoptimal dye concentration at (AgCl 5g/l and dye 5g/l). Antibacterial tests were conducted on the optimal specimens from both methods (AgCl 0.5%, 0.2%, dye 0.5% for exhaust; dye 5g/l, AgCl 5g/l, 2g/l for pad dry cure), showcasing resistance against bacterial growth. While inhibition zones were observed on treated specimens of the exhaust method, whereas the treated specimens of the pad dry cure method exhibited complete resistance to bacterial growth around the specimen.

Assessment of silver and graphitic carbon nitride doped cadmium selenide quantum dots as an efficient dye degrader and antibacterial agent: In silico molecular docking analysis

Assessment of silver and graphitic carbon nitride doped cadmium selenide quantum dots as an efficient dye degrader and antibacterial agent: In silico molecular docking analysis

Unveiling the antibacterial potential of anthocyanins - a comprehensive review on this natural plant extract.

With the gradual prohibition of antibiotic fungicides, it is of great significance to develop high-efficient, nontoxic and environmental-friendly antimicrobial agents. Anthocyanin is a natural plant polyphenol pigment which shows antibacterial, anti-inflammatory and antioxidant effects through inhibiting the synthesis of bacterial cell wall, interfering bacterial respiratory metabolism, and inducing bacterial autolysis. As a typical antibacterial agent, anthocyanins have been widely used in various fields, including biological pesticides or feed additives in agricultural production, anti-inflammatory and antibacterial wound dressings in medicine, etc. However, the structure of anthocyanins is unstable, which limits its practical application. In this article, the biological activity, antibacterial mechanism and stabilization strategy of anthocyanins as antibacterial agents were reviewed. The safety, application scope and methods of anthocyanins were discussed. In addition, the challenges and development prospects of anthocyanin extract antibacterial technology were also prospected. This will be the direction for researchers to further explore and better apply anthocyanins to practical production and application.

Synthesis of cytocompatible gum Arabic-encapsulated silver nitroprusside nanocomposites for inhibition of bacterial pathogens and food safety applications.

Silver nitroprusside (AgN) exhibits significant antibacterial activity; however, its inherent toxicity poses a major concern. This study synthesized AgN with enhanced antibacterial properties while minimizing toxicity. Gum Arabic (GA), a natural polysaccharide widely utilized in food and biomedical applications owing to its exceptional cytocompatibility, was selected for encapsulating AgN to mitigate toxicity while preserving or enhancing its biological activity. The resulting composite material, GA-AgN nanocomposites (NCs), was systematically characterized using various analytical techniques. Transmission electron microscopy analysis revealed that GA-AgN NCs exhibited a rectangular morphology, with an average size of 230.13±62.8nm. The zeta potential of GA-AgN NCs was measured at -29.3±0.70mV. Furthermore, GA-AgN NCs demonstrated stability over diverse storage durations, incubation periods, and pH conditions by maintaining its size and surface charge. X-ray diffraction results indicated a reduction in the crystallinity of AgN when incorporated into the amorphous GA matrix, while Fourier-transform infrared spectroscopy analysis confirmed that the functional properties of both AgN and GA were preserved in the NCs. The release of Ag and Fe ions from the NCs was observed to be time- and pH-dependent. Importantly, the incorporation of GA did not compromise the antibacterial or antibiofilm efficacy of AgN against bacterial pathogens. Additionally, GA significantly mitigated the cytotoxic effects of AgN on NIH3T3 cells and red blood cells. Furthermore, GA-AgN NCs effectively extended the shelf-life of Salmonella enterica-infected green grapes. Thus, this study illustrates that GA-fabricated AgN NCs exhibit potential as an antibacterial agent in food preservation applications.

Synthesis of New Structural Thiosemicarbazones and Investigation of Their Antibacterial Activities Against E. Coli

AbstractThis study focuses on the synthesis and characterization of novel thiosemicarbazone derivatives with potential antibacterial activity. Through a systematic two‐step synthesis process, involving the preparation of substitute aldehydes (A1–A6) followed by the formation of thiosemicarbazone derivatives (S1–S6), novel compounds (S1, S2) were successfully obtained. The structures of the synthesized compounds were thoroughly characterized using FT‐IR, 1H‐NMR, 13C‐NMR, LC/MS, UV‐Vis, and SEM‐EDX. The results highlight the significance of sulfuric acid as a catalyst in the synthesis of pyrazole‐thiosemicarbazide derivatives (S1, S2), demonstrating its superior efficiency compared to acetic acid. The compounds exhibited varying degrees of antibacterial activity against E. coli, with compounds S3–S6 showing promising results with MIC values below 25 mg/mL. These findings indicate the potential of these compounds as antibacterial agents. Overall, the successful synthesis and characterization of these novel derivatives open avenues for further research into their potential pharmacological applications. The findings of this study lay the foundation for future studies aimed at optimizing these compounds for enhanced antimicrobial activity and exploring their therapeutic potential in treating bacterial infections.

Antibacterial properties enhancement tropical fruit waste biopolymer hydrogel loaded Nephelium Lappaceum leaf extract for sanitizing applications.

Current alcohol-based sanitizers present safety concerns and are not suitable for all applications. To address the issue, biopolymer hydrogels offer a safer, sustainable alternative due to biocompatibility, biodegradability, and customizable properties. In present study, carboxymethyl cellulose (CMC) was prepared from Durian fruit rind, a tropical fruit byproduct rich in polysaccharides and combined with the synthetic polymer Carbopol to form a hydrogel with homogenization technique. Rambutan (Nephelium lappaceum) leaf extract (RLE) as an antibacterial agent was analyzed for functional, morphological, antibacterial, and structural properties. Phytochemical analysis of RLE confirmed the presence of antibacterial compounds, while Minimum Inhibitory Concentrations (MIC) were 33.3μg/mL for Escherichia coli and 28.5μg/mL for Staphylococcus aureus. Additionally, Scanning Electron Microscopy showed significant disruptions in bacterial cell walls. Hydrogel incorporated RLE was produced with improved properties confirmed through viscosity, FT-IR, Disc-diffusion assay and spread plate method analysis. In general, Rambutan leaf extract significantly improves the antibacterial properties of biopolymer-based hydrogels, hence offering a promising, eco-friendly alternative to alcohol-based sanitizers.

Preparation and characterization of an antibacterial CMC/PCL hydrogel films containing CIP/Cur: In vitro and in vivo evaluation of wound healing activity

Wound healing process significantly impeded by prolonged inflammation responses, infection at the wound site, and insufficient angiogenesis. The sustained release of anti-inflammation and anti-bacterial drugs has the potential to control immune responses, improve angiogenesis, accelerate wound healing, and re-epithelialization. In this research a multifunctional hydrogel containing carboxy methyl cellulose (CMC) and polycaprolactone (PCL), along with Ciprofloxacin (CIP) and Curcumin (Cur) was developed. Physicochemical characteristics as well a biological one such as antibacterial and drug release properties, Collagen deposition, inflammatory responses, angiogenesis, and epidermal regenerated thickness were investigated via in vitro and in vivo assay. The results revealed that the CMC/PCL-based wound dressing has the potential to provide an appropriate level of water absorption (~300 %) to absorb wound exudate and ideal WVTR in range of 2279–2363 g/m2 for wound healing application. Addition of CIP and Cur to CMC/PCL hydrogel improved the skin cell proliferation, cell migration, and antibacterial activity. It also led to superior Collagen I synthesis (~2–4 times), controlled pro-inflammatory and improved anti-inflammatory cytokine secretion of macrophages, and accelerated wound healing in comparison to CMC/PCL hydrogel. In conclusion, the engineered multifunctional hydrogel showed a potential effect for accelerating wound healing and skin regeneration.

Antibacterial profile and antiproliferative activities over human tumor cells of new silver(I) complexes containing two distinct trifluoromethyl uracil isomers

New silver(I) complexes of 5-(trifluoromethyl)uracil (5TFMU) and 6-(trifluoromethyl)uracil (6TFMU) isomers were synthesized, characterized, and evaluated as antibacterial and antiproliferative agents. Based on elemental and thermogravimetric analyses, the Ag-5TFMU and Ag-6TFMU species are formulated as AgC5H2F3N2O2 and Ag2C5HF3N2O2, respectively. Infrared and 13C solid-state nuclear magnetic resonance spectroscopies suggest coordination of the trifluoromethyluracil isomers to silver by both nitrogen and oxygen atoms. Confirmation of their structure and connectivity was achieved, in the absence of single crystals of suitable quality, by state-of-the-art structural powder diffraction methods. In Ag-5TFMU, the organic ligand is tridentate and two distinct metal coordination environments are found (linear AgN2 as well as C2v AgO4 geometries), whereas Ag-6TFMU contains a complex polymeric structure with tetradentate dianionic 6TFMU moieties and five distinct AgX2 (X = N, O) fragments, further stabilized by ancillary (longer) Ag…O contacts. These species presented modest activity over Gram-positive and Gram-negative bacterial strains, whereas Ag-6TFMU was active over a set of tumor cells, with the best activity over prostate (PC-3) and kidney cell lines and selectivity indices of 4.6 and 1.3, respectively. On the other hand, Ag-5TFMU was active over all considered tumor cells except MCF-7 (breast cancer). The best activity was found for PC-3 cells, but no selectivity was observed. The Ag-5TFMU and Ag-6TFMU species also reduced the proliferation of tongue squamous cell carcinoma cell lines SCC − 4 and SCC-15. Preliminary biophysical assays by circular dichroism suggest that the Ag-5TFMU complex interacts with DNA by intercalation, an effect not seen in Ag-6TFMU.