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Article

Synthesis and Physicochemical Characterization of Novel Dicyclopropyl-Thiazole Compounds as Nontoxic and Promising Antifungals

1
Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University of Lublin, Chodźki 1, 20-093 Lublin, Poland
2
Department of Chemical Technology and Pharmaceuticals, Faculty of Pharmacy, Collegium Medicum, Nicolaus Copernicus University, Jurasza 2, 85-089 Bydgoszcz, Poland
3
Department of Molecular Biology, Faculty of Science and Health, The John Paul II Catholic University of Lublin, Konstantynów 1i, 20-708 Lublin, Poland
4
Institute of Physics, Kazimierz Wielki University, Powstańców Wielkopolskich 2, 85-090 Bydgoszcz, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Alina Maria Holban
Materials 2021, 14(13), 3500; https://doi.org/10.3390/ma14133500
Received: 1 May 2021 / Revised: 24 May 2021 / Accepted: 10 June 2021 / Published: 23 June 2021
(This article belongs to the Special Issue Novel Materials for Antimicrobial Application)
There is a need to search for new antifungals, especially for the treatment of the invasive Candida infections, caused mainly by C. albicans. These infections are steadily increasing at an alarming rate, mostly among immunocompromised patients. The newly synthesized compounds (3a3k) were characterized by physicochemical parameters and investigated for antimicrobial activity using the microdilution broth method to estimate minimal inhibitory concentration (MIC). Additionally, their antibiofilm activity and mode of action together with the effect on the membrane permeability in C. albicans were investigated. Biofilm biomass and its metabolic activity were quantitatively measured using crystal violet (CV) staining and tetrazolium salt (XTT) reduction assay. The cytotoxic effect on normal human lung fibroblasts and haemolytic effect were also evaluated. The results showed differential activity of the compounds against yeasts (MIC = 0.24–500 µg/mL) and bacteria (MIC = 125–1000 µg/mL). Most compounds possessed strong antifungal activity (MIC = 0.24–7.81 µg/mL). The compounds 3b, 3c and 3e, showed no inhibitory (at 1/2 × MIC) and eradication (at 8 × MIC) effect on C. albicans biofilm. Only slight decrease in the biofilm metabolic activity was observed for compound 3b. Moreover, the studied compounds increased the permeability of the membrane/cell wall of C. albicans and their mode of action may be related to action within the fungal cell wall structure and/or within the cell membrane. It is worth noting that the compounds had no cytotoxicity effect on pulmonary fibroblasts and erythrocytes at concentrations showing anticandidal activity. The present studies in vitro confirm that these derivatives appear to be a very promising group of antifungals for further preclinical studies. View Full-Text
Keywords: antifungal activity; Candida albicans; antibiofilm effect; mode of action; cytotoxicity; haemolytic assay; HOMO–LUMO; molecular electrostatic potential antifungal activity; Candida albicans; antibiofilm effect; mode of action; cytotoxicity; haemolytic assay; HOMO–LUMO; molecular electrostatic potential
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MDPI and ACS Style

Biernasiuk, A.; Banasiewicz, A.; Masłyk, M.; Martyna, A.; Janeczko, M.; Baranowska-Łączkowska, A.; Malm, A.; Łączkowski, K.Z. Synthesis and Physicochemical Characterization of Novel Dicyclopropyl-Thiazole Compounds as Nontoxic and Promising Antifungals. Materials 2021, 14, 3500. https://doi.org/10.3390/ma14133500

AMA Style

Biernasiuk A, Banasiewicz A, Masłyk M, Martyna A, Janeczko M, Baranowska-Łączkowska A, Malm A, Łączkowski KZ. Synthesis and Physicochemical Characterization of Novel Dicyclopropyl-Thiazole Compounds as Nontoxic and Promising Antifungals. Materials. 2021; 14(13):3500. https://doi.org/10.3390/ma14133500

Chicago/Turabian Style

Biernasiuk, Anna, Anna Banasiewicz, Maciej Masłyk, Aleksandra Martyna, Monika Janeczko, Angelika Baranowska-Łączkowska, Anna Malm, and Krzysztof Z. Łączkowski 2021. "Synthesis and Physicochemical Characterization of Novel Dicyclopropyl-Thiazole Compounds as Nontoxic and Promising Antifungals" Materials 14, no. 13: 3500. https://doi.org/10.3390/ma14133500

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