Antifungal activity’s study of the of new derivatives of pyrrolo[3,4-c]pyrazol-3-ones and pyrazol-3- carboxamides in the biofilm model of Candida spp.

The search for new antifungal drugs is current interest due to the wide spread of fungal infections. To simulate the antifungal effect of new promising compounds with high antifungal activity in planktonic culture in clinical practice, it is necessary to study their effect on the biofilm of micromycetes. Aim: To study the antifungal activity of new promising representatives of silver salts of pyrazoles and their condensed systems under conditions of biofilm formation. Material and Methods. To study the antifungal activity of silver salts I and II, the micromethod of two-fold serial dilutions was used. Activity against a typical and 14 clinical highly virulent isolates of C. albicans was studied. The study of the antimycotic activity of substances under biofilm conditions was carried out using resazurin to quantify the degree of biofilm formation. The minimum inhibitory concentrations for biofilms were calculated (sMIC50 - the concentration of the antifungal substance at which a 50% decrease in fluorescence is observed compared to the positive control). Results and Discussion. It was shown that the antifungal effect of the studied compounds in biofilm culture of clinical strains of Candida spp. is significantly lower than in planktonic culture. High antifungal activity of the silver salt of pyrazole-3- carboxamide in planktonic and biofilm cultures of resistant strains of Candida albicans, exceeding the effect of the reference drug fluconazole by 2.8–11.2 times, was revealed. Conclusion. A promising pyrazole-3-carboxamide derivative has been identified that effectively inhibits the growth of Candida albicans biofilms, which can be recommended for further study.

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Publication Details

Journal
Siberian Journal of Clinical and Experimental Medicine
Published
2024-10-02
DOI
https://doi.org/10.29001/2073-8552-2024-39-3-150-155
Primary Topic
Antifungal resistance and susceptibility
Type
article
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article

Antifungal activity’s study of the of new derivatives of pyrrolo[3,4-c]pyrazol-3-ones and pyrazol-3- carboxamides in the biofilm model of Candida spp.

В. В. Новикова, В. Л. Гейн, O. V. Bobrovskaya
Siberian Journal of Clinical and Experimental Medicine
Antifungal resistance and susceptibility
article

Antifungal activity’s study of the of new derivatives of pyrrolo[3,4-c]pyrazol-3-ones and pyrazol-3- carboxamides in the biofilm model of Candida spp.

В. В. Новикова, В. Л. Гейн, O. V. Bobrovskaya
article en

Abstract

The search for new antifungal drugs is current interest due to the wide spread of fungal infections. To simulate the antifungal effect of new promising compounds with high antifungal activity in planktonic culture in clinical practice, it is necessary to study their effect on the biofilm of micromycetes. Aim: To study the antifungal activity of new promising representatives of silver salts of pyrazoles and their condensed systems under conditions of biofilm formation. Material and Methods. To study the antifungal activity of silver salts I and II, the micromethod of two-fold serial dilutions was used. Activity against a typical and 14 clinical highly virulent isolates of C. albicans was studied. The study of the antimycotic activity of substances under biofilm conditions was carried out using resazurin to quantify the degree of biofilm formation. The minimum inhibitory concentrations for biofilms were calculated (sMIC50 - the concentration of the antifungal substance at which a 50% decrease in fluorescence is observed compared to the positive control). Results and Discussion. It was shown that the antifungal effect of the studied compounds in biofilm culture of clinical strains of Candida spp. is significantly lower than in planktonic culture. High antifungal activity of the silver salt of pyrazole-3- carboxamide in planktonic and biofilm cultures of resistant strains of Candida albicans, exceeding the effect of the reference drug fluconazole by 2.8–11.2 times, was revealed. Conclusion. A promising pyrazole-3-carboxamide derivative has been identified that effectively inhibits the growth of Candida albicans biofilms, which can be recommended for further study.

Siberian Journal of Clinical and Experimental MedicineVol. 39(3)
Ministry of Health of the Russian Federation (RU), Perm State Pharmaceutical Academy (RU)
Openalex Percentile: Top 78%
Antifungal resistance and susceptibility
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