A highly substituted and fluorescent aromatic-fused imidazole derivative that shows enhanced antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA)

Bulut, Onur; Öktem, Hüseyin Avni; Yilmaz, M. Deniz

doi:10.1016/j.jhazmat.2020.122902

Cited by 18 publications

(8 citation statements)

References 44 publications

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“…They are known to inhibit the synthesis of ergosterol, the main sterol of fungal membranes, as well as other important components [26,27]. Imidazoles are currently the focus of numerous medicinal chemistry efforts and many derivatives have shown potent antibacterial and anti-biofilm activity [28][29][30][31]. Therefore, it is not surprising that they were also identified as positive hits in our study.…”

Section: Hit-to-lead Identification Processmentioning

confidence: 58%

Screening of FDA-Approved Drugs Using a 384-Well Plate-Based Biofilm Platform: The Case of Fingolimod

et al. 2020

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In an effort to find new repurposed antibacterial compounds, we performed the screening of an FDA-approved compounds library against Staphylococcus aureus American Type Culture Collection (ATCC) 25923. Compounds were evaluated for their capacity to prevent both planktonic growth and biofilm formation as well as to disrupt pre-formed biofilms. One of the identified initial hits was fingolimod (FTY720), an immunomodulator approved for the treatment of multiple sclerosis, which was then selected for follow-up studies. Fingolimod displayed a potent activity against S. aureus and S. epidermidis with a minimum inhibitory concentration (MIC) within the range of 12–15 µM at which concentration killing of all the bacteria was confirmed. A time–kill kinetic study revealed that fingolimod started to drastically reduce the viable bacterial count within two hours and we showed that no resistance developed against this compound for up to 20 days. Fingolimod also displayed a high activity against Acinetobacter baumannii (MIC 25 µM) as well as a modest activity against Escherichia coli and Pseudomonas aeruginosa. In addition, fingolimod inhibited quorum sensing in Chromobacterium violaceum and might therefore target this signaling pathway in certain Gram-negative bacteria. In conclusion, we present the identification of fingolimod from a compound library and its evaluation as a potential repurposed antibacterial compound.

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Section: Hit-to-lead Identification Processmentioning

confidence: 58%

Screening of FDA-Approved Drugs Using a 384-Well Plate-Based Biofilm Platform: The Case of Fingolimod

et al. 2020

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“…Interestingly, A. mali FL18 became resistant to all the antibiotics tested, except to chloramphenicol and tetracycline. The MIC values determined against ampicillin, erythromycin, kanamycin, streptomycin, and vancomycin were comparable to those of other antibiotic-resistant bacteria, as well as those relative to bacitracin (700 µg/ml) and ciprofloxacin (up to 1 mg/ml) (D'Aimmo et al, 2007;Minarini et al, 2012;Bulut et al, 2020). Besides the putative gene coding for BcrC and possibly responsible for bacitracin resistance (see above), it can be hypothesized that the expression of several multidrug-efflux transporters (Table 5) is responsible for the resistance to the other tested antibiotics.…”

Section: Antibiotic Susceptibility In a Mali Fl18mentioning

confidence: 58%

Genomic Insight of Alicyclobacillus mali FL18 Isolated From an Arsenic-Rich Hot Spring

et al. 2021

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Extreme environments are excellent places to find microorganisms capable of tolerating extreme temperature, pH, salinity pressure, and elevated concentration of heavy metals and other toxic compounds. In the last decades, extremophilic microorganisms have been extensively studied since they can be applied in several fields of biotechnology along with their enzymes. In this context, the characterization of heavy metal resistance determinants in thermophilic microorganisms is the starting point for the development of new biosystems and bioprocesses for environmental monitoring and remediation. This work focuses on the isolation and the genomic exploration of a new arsenic-tolerant microorganism, classified as Alicyclobacillus mali FL18. The bacterium was isolated from a hot mud pool of the solfataric terrains in Pisciarelli, a well-known hydrothermally active zone of the Campi Flegrei volcano near Naples in Italy. A. mali FL18 showed a good tolerance to arsenite (MIC value of 41 mM), as well as to other metals such as nickel (MIC 30 mM), cobalt, and mercury (MIC 3 mM and 17 μM, respectively). Signatures of arsenic resistance genes (one arsenate reductase, one arsenite methyltransferase, and several arsenite exporters) were found interspersed in the genome as well as several multidrug resistance efflux transporters that could be involved in the export of drugs and heavy metal ions. Moreover, the strain showed a high resistance to bacitracin and ciprofloxacin, suggesting that the extreme environment has positively selected multiple resistances to different toxic compounds. This work provides, for the first time, insights into the heavy metal tolerance and antibiotic susceptibility of an Alicyclobacillus strain and highlights its putative molecular determinants.

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“…Particularly, the PVDF‐2 membrane performed much better against E. coli and S. aureus strains. The multiple pathways relating to zinc and imidazole involvement in antibacterial activity have been reported 57,58 . The zinc and imidazole could bind to the cell membrane of bacteria and possibly destroy the strain's arrangement.…”

Section: Resultsmentioning

confidence: 99%

Development of highly permeable and antifouling poly(vinylidene fluoride) hybrid membranes tailored with ZIF‐8 metal–organic frameworks for water treatment

Rameesha

Rana

Nagendran

2023

Polymers for Advanced Techs

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This study deals with the making of poly(vinylidene fluoride) (PVDF) hybrid ultrafiltration (UF) membranes incorporated with zeolitic imidazolate framework-8 (ZIF-8) nanocrystals. The surface morphology and roughness of ZIF-8 are explored in terms of atomic force microscopy (AFM) and scanning electron microscopy (SEM) whereas their distribution in PVDF matrix and antibacterial activity are probed by energy dispersive X-ray (EDX) analysis and zone of inhibition test. The chemical functionality of ZIF-8 is verified by Fourier transform infrared (FTIR) and X-ray diffraction (XRD) spectroscopic studies. The permeability of hybrid membranes is raised to 2 wt% addition of ZIF-8 into the PVDF matrix owing to an enhancement in hydrophilicity and porosity. The FESEM images of the top and cross-section view make visible the formation of macrovoids with the addition of ZIF-8. On account of high porosity and surface hydrophilicity, the pure water permeation of hybrid membranes is increased to 278.6 Lm À2 h À1 . The hybrid membranes showed higher rejection and permeate flux of bovine serum albumin (BSA; 92.8 Lm À2 h À1 ) and humic acid (HA; 94.3 Lm À2 h À1 ) owing to the synergetic effect of their enhanced hydrophilicity and surface roughness. This is confirmed by the higher flux recovery ratio (FRR) and lower irreversible fouling characteristics of hybrid PVDF membranes. The atomic absorption spectroscopy (AAS) revealed the long-standing stability of ZIF-8 in the PVDF matrix. Among all, the PVDF hybrid membrane with 2 wt% of ZIF-8 showed excellent permeability, antifouling, and antibiofouling ability and was found to be more effective in water treatment applications.

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A highly substituted and fluorescent aromatic-fused imidazole derivative that shows enhanced antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA)

Cited by 18 publications

References 44 publications

Screening of FDA-Approved Drugs Using a 384-Well Plate-Based Biofilm Platform: The Case of Fingolimod

Screening of FDA-Approved Drugs Using a 384-Well Plate-Based Biofilm Platform: The Case of Fingolimod

Genomic Insight of Alicyclobacillus mali FL18 Isolated From an Arsenic-Rich Hot Spring

Development of highly permeable and antifouling poly(vinylidene fluoride) hybrid membranes tailored with ZIF‐8 metal–organic frameworks for water treatment

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