Design, synthesis, and biological evaluation of novel boron-containing azoles as potential antifungal agents

Yan, Zhong-zuo; Lv, Z.; Guo, Mengbi; Wang, Yitong; Hou, Zhuang; Guo, Chun

doi:10.1016/j.molstruc.2023.135997

Cited by 3 publications

(4 citation statements)

References 16 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The experiments using transmission electron microscopy are based on prior research but with some changes C.…”

Section: Methodsmentioning

confidence: 99%

“…We carried out the GC-MS analysis using the previously described methodology. , Candida albicans (SC5314) was selected as the model strain in this experiment.…”

Section: Methodsmentioning

confidence: 99%

“…The experiments using transmission electron microscopy are based on prior research but with some changes. 33 C. albicans SC5314 was used as a test strain, while fluconazole was selected as a positive control. Added was 16 μg/mL of FLU final concentration, 16 μg/mL of A32 final concentration, and DMSO as a blank control to the fungal solution at 30 °C, 200 rpm, shaking incubation for 24 h. The fungus solution is then centrifuged, saline-washed three times, given an electron microscope fixative, and allowed to be static at room temperature for 2 h. Transmission electron microscopy was used to view and take pictures of the treated samples, and the results were evaluated.…”

Section: -Methoxy-3-((1-(24-difluorophenyl)-2-(1h-imidazol-1-yl)ethox...mentioning

confidence: 99%

“…The cytotoxicity assay was performed by us using the previously described methods. 33 The human embryonic lung fibroblast (MRC-5) and mouse mononuclear macrophage (J774A.1) were chosen as tested cell lines.…”

Section: -Methoxy-3-((1-(24-difluorophenyl)-2-(1h-imidazol-1-yl)ethox...mentioning

confidence: 99%

See 3 more Smart Citations

Developing Novel Coumarin-Containing Azoles Antifungal Agents by the Scaffold Merging Strategy for Treating Azole-Resistant Candidiasis

Yan,

Huang,

Zhao

et al. 2023

J. Med. Chem.

Self Cite

View full text Add to dashboard Cite

The extensive use of antifungal drugs has resulted in severe drug resistance, making clinical treatment of fungal infections more difficult. Biofilm inhibitors can overcome drug resistance by inhibiting fungal biofilm formation. In this study, some coumarins with antibiofilm activity were merged into CYP51 inhibitors to produce novel molecules possessing potent antiresistance activity. As expected, most compounds exhibited excellent in vitro antifungal activity against pathogenic fungi, especially fluconazole-resistant candidiasis. Then, their mechanism was confirmed by sterol composition analysis and morphological observation. Biofilm inhibition and down-regulation of resistancerelated genes were employed to confirm the compounds' antiresistance mechanisms. Significantly, compound A32 demonstrated fungicidal activity against fluconazole-resistant strain 904. Most importantly, compound A32 showed potent in vivo antifungal activity against pathogenic fungi and fluconazole-resistant strains. Preliminary pharmacokinetic and toxicity tests demonstrated that the compounds possessed favorable druggability. Taken together, compound A32 represents a promising lead to develop novel antifungal agents for treating azole-resistant candidiasis.

show abstract

“…The experiments using transmission electron microscopy are based on prior research but with some changes C.…”

Section: Methodsmentioning

confidence: 99%

“…We carried out the GC-MS analysis using the previously described methodology. , Candida albicans (SC5314) was selected as the model strain in this experiment.…”

Section: Methodsmentioning

confidence: 99%

Section: -Methoxy-3-((1-(24-difluorophenyl)-2-(1h-imidazol-1-yl)ethox...mentioning

confidence: 99%

Section: -Methoxy-3-((1-(24-difluorophenyl)-2-(1h-imidazol-1-yl)ethox...mentioning

confidence: 99%

See 2 more Smart Citations