NO<sub>2</sub>‐Fe (II)Pc‐catalyzed synthesis of 2‐ferrocenyl‐5‐aryl‐1,3,4‐oxadiazoles and study of antifungal activity

Ge, Man; Feng, Jie; Huang, Huiping; Gou, Xin; Hua, Chengwen; Chen, Bang; Zhao, Jihe

doi:10.1002/jhet.3725

Cited by 3 publications

(4 citation statements)

References 39 publications

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“…Both 18b and 18e can be considered as promising drugs for further investigation. 58 Recently, four FCZ ferrocenyl derivatives with one triazole moiety replaced by different alkyl substituents were developed in our group. The stability of these complexes in deuterated DMSO and H 2 O -common media for preparation of stock solutions for biological screeningwere monitored by NMR spectroscopy and showed that all tested compounds were stable for up to 24 hours in solution.…”

Section: Metallocenyl-derivatives Of Azole Antifungal Drugsmentioning

confidence: 99%

Recent developments of metal-based compounds against fungal pathogens

et al. 2021

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Section: Metallocenyl-derivatives Of Azole Antifungal Drugsmentioning

confidence: 99%

Recent developments of metal-based compounds against fungal pathogens

et al. 2021

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“…One issue that the authors noted, in addition to the small number of systematic studies into antifungal metal complexes, is the lack of mode of action studies and the often less than ideal antifungal data collection and reporting with regard to methodology and controls. Furthermore, there are only a few studies reporting in vivo evaluation of antifungal metal-based compounds. ,,,,, A series of phenanthroline complexes containing copper, manganese, or silver showed no toxicity in a G. mellonella (moth larvae) in vivo model at 10 μg/larva, and most complexes reduced the fungal burden of larvae infected with Candida haemulonii. , Silver complexes of 1,10-phenanthroline-5,6-dione protected G.…”

Section: Introductionmentioning

confidence: 99%

“…Furthermore, there are only a few studies reporting in vivo evaluation of antifungal metal-based compounds. 28,30,35,51,53,54 A series of phenanthroline complexes containing copper, manganese, or silver showed no toxicity in a G. mellonella (moth larvae) in vivo model at 10 μg/larva, and most complexes reduced the fungal burden of larvae infected with Candida haemulonii. 41,53 Silver complexes of 1,10-phenanthroline-5,6-dione protected G. mellonella larvae from infection with Phialophora verrucose.…”

Section: ■ Introductionmentioning

confidence: 99%

Metal Complexes as Antifungals? From a Crowd-Sourced Compound Library to the First In Vivo Experiments

Frei

Elliott

Kan

et al. 2022

JACS Au

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There are currently fewer than 10 antifungal drugs in clinical development, but new fungal strains that are resistant to most current antifungals are spreading rapidly across the world. To prevent a second resistance crisis, new classes of antifungal drugs are urgently needed. Metal complexes have proven to be promising candidates for novel antibiotics, but so far, few compounds have been explored for their potential application as antifungal agents. In this work, we report the evaluation of 1039 metal-containing compounds that were screened by the Community for Open Antimicrobial Drug Discovery (CO-ADD). We show that 20.9% of all metal compounds tested have antimicrobial activity against two representative Candida and Cryptococcus strains compared with only 1.1% of the >300,000 purely organic molecules tested through CO-ADD. We identified 90 metal compounds (8.7%) that show antifungal activity while not displaying any cytotoxicity against mammalian cell lines or hemolytic properties at similar concentrations. The structures of 21 metal complexes that display high antifungal activity (MIC ≤1.25 μM) are discussed and evaluated further against a broad panel of yeasts. Most of these have not been previously tested for antifungal activity. Eleven of these metal complexes were tested for toxicity in the Galleria mellonella moth larva model, revealing that only one compound showed signs of toxicity at the highest injected concentration. Lastly, we demonstrated that the organo-Pt(II) cyclooctadiene complex Pt1 significantly reduces fungal load in an in vivo G. mellonella infection model. These findings showcase that the structural and chemical diversity of metal-based compounds can be an invaluable tool in the development of new drugs against infectious diseases.

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“…Only a couple of studies so far have reported the in vivo evaluation of metal-based compounds. 28,30,35,51,[53][54] Gandra et al studied a series of phenanthroline complexes containing copper, manganese and silver. They demonstrated that these compounds showed no toxicity in a Galleria mellonella (moth larvae) in vivo model at 10 µg/larva.…”

Section: Introductionmentioning

confidence: 99%

Metal Complexes as Antifungals? – From a Crowd-Sourced Compound Library to First In Vivo Experiments

Frei

Elliott

Kan

et al. 2022

Preprint

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There are currently fewer than ten antifungal drugs in clinical development, but new fungal strains, which are resistant to most current antifungals are spreading rapidly across the world. To prevent a second resistance crisis, new classes of antifungal drugs are urgently needed. Metal complexes have proven to be promising candidates for novel antibiotics, but so far, few compounds have been explored for their potential application as antifungal agents. In this work we report the evaluation of 1039 metal-containing compounds that were screened by the Community for Open Antimicrobial Drug Discovery (CO-ADD). We show that 20.9% of all metal compounds tested have antimicrobial activity against two representative Candida and Cryptococcus strains, compared with only 1.1% of the >300,000 purely organic molecules tested through CO-ADD. We identified 90 metal compounds (8.7%) that show antifungal activity while not displaying any cytotoxicity against mammalian cell lines or haemolytic properties at similar concentrations. The structures of 21 metal complexes which display high antifungal activity (MIC ≤ 1.25 µM) are discussed and evaluated further against a broad panel of yeasts. Most of these have not been evaluated for antifungal activity. Eleven of these metal complexes were tested for toxicity in the Galleria mellonella moth larvae model, revealing that only one compound showed signs of toxicity at the highest injected concentration. Lastly, we demonstrated that the organo-Pt(II) cyclooctadiene complex Pt1 significantly reduces fungal load in an in vivo G. mellonella infection model. These findings showcase that the structural and chemical diversity of metal-based compounds can be an invaluable tool in the development of new drugs against infectious diseases.

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NO₂‐Fe (II)Pc‐catalyzed synthesis of 2‐ferrocenyl‐5‐aryl‐1,3,4‐oxadiazoles and study of antifungal activity

Cited by 3 publications

References 39 publications

Recent developments of metal-based compounds against fungal pathogens

Recent developments of metal-based compounds against fungal pathogens

Metal Complexes as Antifungals? From a Crowd-Sourced Compound Library to the First In Vivo Experiments

Metal Complexes as Antifungals? – From a Crowd-Sourced Compound Library to First In Vivo Experiments

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NO2‐Fe (II)Pc‐catalyzed synthesis of 2‐ferrocenyl‐5‐aryl‐1,3,4‐oxadiazoles and study of antifungal activity

Cited by 3 publications

References 39 publications

Recent developments of metal-based compounds against fungal pathogens

Recent developments of metal-based compounds against fungal pathogens

Metal Complexes as Antifungals? From a Crowd-Sourced Compound Library to the First In Vivo Experiments

Metal Complexes as Antifungals? – From a Crowd-Sourced Compound Library to First In Vivo Experiments

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NO₂‐Fe (II)Pc‐catalyzed synthesis of 2‐ferrocenyl‐5‐aryl‐1,3,4‐oxadiazoles and study of antifungal activity