Novel avenues for identification of new antifungal drugs and current challenges

Jampílek, Josef

doi:10.1080/17460441.2022.2097659

Cited by 6 publications

(5 citation statements)

References 219 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Phenothiazines are also known for their ability to interact with and damage the cell wall, which has fatal consequences for the microorganism [ 44 , 45 ]. Therefore, the bacterial suspensions were treated by compounds 6a , 6e , 6g , 6j and 6k (4× MIC) for 1 h. The uptake of crystal violet was expressed as a percentage compared to the original crystal violet solution.…”

Section: Resultsmentioning

confidence: 99%

“…Phenothiazines, like quinolines, are multi-target agents, i.e., they have the ability to affect several different targets, leading to the death of treated microorganisms. Quinolines are known to be able to inhibit, for example, the respiratory chain (possessing a similar mechanism of action to bedaquiline [ 46 , 47 , 48 , 49 ]), sulphur metabolic pathways [ 50 ] or mycobacterial FtsZ protein [ 51 ]; phenothiazines, in addition to the aforementioned ability to interact with the bacterial membrane, have the ability to inhibit the respiratory chain, dissipate the membrane potential, reduce the level of ATP, increase oxidative stress or increase the level of intracellular ions [ 44 , 45 , 52 , 53 ].…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Design, Synthesis and Antimicrobial Properties of New Tetracyclic Quinobenzothiazine Derivatives

Kisiel-Nawrot

Pindjakova²,

Latocha³

et al. 2022

IJMS

Self Cite

View full text Add to dashboard Cite

A new method for modifying the structure of tetracyclic quinobenzothiazinium derivatives has been developed, allowing introduction of various substituents at different positions of the benzene ring. The method consists of reacting appropriate aniline derivatives with 5,12-(dimethyl)thioquinantrenediinium bis-chloride. A series of new quinobenzothiazine derivatives was obtained with propyl, allyl, propargyl and benzyl substituents in 9, 10 and 11 positions, respectively. The structure of the obtained compounds was analyzed by 1H and 13C NMR (HSQC, HMBC) and X-ray analysis. All the compounds were tested against reference strains Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212, and representatives of multidrug-resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant E. faecalis (VRE). In addition, all the compounds were evaluated in vitro against Mycobacterium smegmatis ATCC 700084 and M. marinum CAMP 5644. 9-Benzyloxy-5-methyl-12H-quino [3,4-b][1,4]benzothiazinium chloride (6j), 9-propoxy-5-methyl-12H-quino[3,4-b][1,4]benzothiazinium chloride (6a) and 9-allyloxy-5-methyl-12H-quino[3,4-b][1,4]benzothiazinium chloride (6d) demonstrated high activity against the entire tested microbial spectrum. The activities of the compounds were comparable with oxacillin, tetracycline and ciprofloxacinagainst staphylococcal strains and with rifampicin against both mycobacterial strains. Compound 6j had a significant effect on the inhibition of bacterial respiration as demonstrated by the MTT assay. The compounds showed not only bacteriostatic activity, but also bactericidal activity. Preliminary in vitro cytotoxicity screening of the compounds performed using normal human dermal fibroblasts (NHDF) proved that the tested compounds showed an insignificant cytotoxic effect on human cells (IC50 > 37 µM), making these compounds interesting for further investigation. Moreover, the intermolecular similarity of novel compounds was analyzed in the multidimensional space (mDS) of the structure/property-related in silico descriptors by means of principal component analysis (PCA) and hierarchical clustering analysis (HCA), respectively. The distance-oriented structure/property distribution was related with the experimental lipophilic data.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Design, Synthesis and Antimicrobial Properties of New Tetracyclic Quinobenzothiazine Derivatives

Kisiel-Nawrot

Pindjakova²,

Latocha³

et al. 2022

IJMS

Self Cite

View full text Add to dashboard Cite

show abstract

“…The C. albicans strains were cultured on Sabouraud Dextrose Agar plates with a sterile swab moistened with the fungal suspension at 0.5 McFarland. Subsequently, wells of 8 mm diameter were punched into the agar medium and filled with 100 μl (25 mg/ml) of the saturated ([Met-HCl] [PyS]) IL and some ILs composed of other amino acids, allowed to diffuse at room temperature for 2 h. The plates were incubated at 37°C for 24 h. After incubation, the diameters of the growth inhibition zones were measured ( 23 ).…”

Section: Methodsmentioning

confidence: 99%

Effect of new methionine-based ionic liquid on the CDR1 and CDR2 gene expression on sensitive and resistant strains of Candida albicans

Eslami

Ezabadi

Bayat

et al. 2023

IJM

View full text Add to dashboard Cite

Background and Objectives: Previous researchers showed the antimicrobial ability of ionic liquids (ILs) on different infec- tive agents. ILs can dissolve organic components, especially DNA molecules. Among synthesized eight binary ILs mixtures, we have chosen ([Met-HCl] [PyS]) IL for determining the antifungal ability of IL against Candida albicans cells. Materials and Methods: Well diffusion assay, chrome agar and Germ tube tests were used to detect the Candida samples. PCR, real-time-PCR, and flow cytometry tests were performed to determine the IL's rate of toxic ability. Results: Well diffusion assay revealed the diameters of the growth inhibition zones were the largest in IL with methionine and Proline amino acids. Minimum inhibitory concentration (MIC) and the Minimum fungicidal concentration (MFC) tests showed that they inhibited the growth of the C. albicans at a range from 250 µg/ml for sensitivity and 400 µg/ml for resis- tance, MIC average of all samples were 341.62 ± 4.153 µg/ml. IL reduced the expression of CDR1 and CDR2 the genes encoded by the major protein of ABC system transporter by 2.1 (P= 0.009) and 1.2 fold (P= 0.693), revealed by PCR and real time-PCR. In the flow cytometry test, there were increasing dead cells after treating with the ([Met-HCl] [PyS]) even in the most resistant strain. Conclusion: The novel IL was effective against the most clinical and standard C. albicans.

show abstract

“…Currently, the application of chemical fungicides remains the main approach to controlling variety of plant diseases due to their broad‐spectrum, high‐efficiency and low‐cost [3] . However, the prolonged and excessive usage of chemical fungicides has led to a rapidly increasing in pathogen resistance and environment pollution [4] . Therefore, the development of more effective and environment‐friendly small‐molecule fungicides is imminent.…”

Section: Introductionmentioning

confidence: 99%

“…[3] However, the prolonged and excessive usage of chemical fungicides has led to a rapidly increasing in pathogen resistance and environment pollution. [4] Therefore, the development of more effective and environment-friendly small-molecule fungicides is imminent.…”

Section: Introductionmentioning

confidence: 99%

Natural Products‐Based Fungicides: Synthesis and Antifungal Activity against Plant Pathogens of 2H‐Chromene Derivatives

Liu

Fan

et al. 2022

Chemistry & Biodiversity

View full text Add to dashboard Cite

Aiming to search for novel potential antifungal agents, forty 2H‐chromene analogs were designed, synthesized and their antifungal activity against some typical plant pathogenic fungi were firstly evaluated. The in vitro antifungal bioassays showed that some of the target compounds exhibited comparable or better inhibition activities than the commercial agricultural fungicide hymexazol. Especially compound 1m displayed more promising fungicidal effect against Alternaria alternate (EC50=9.9 μg/mL) and Botrytis cinerea (EC50=9.4 μg/mL), which was significantly superior to hymexazol. Moreover, in vivo protective effects results also indicated that compound 1m had an excellent potential for further development as a new botanical pesticide.

show abstract

Novel avenues for identification of new antifungal drugs and current challenges

Cited by 6 publications

References 219 publications

Design, Synthesis and Antimicrobial Properties of New Tetracyclic Quinobenzothiazine Derivatives

Design, Synthesis and Antimicrobial Properties of New Tetracyclic Quinobenzothiazine Derivatives

Effect of new methionine-based ionic liquid on the CDR1 and CDR2 gene expression on sensitive and resistant strains of Candida albicans

Natural Products‐Based Fungicides: Synthesis and Antifungal Activity against Plant Pathogens of 2H‐Chromene Derivatives

Contact Info

Product

Resources

About