The Antifungal Action Mode of N-Phenacyldibromobenzimidazoles

The Antifungal Action Mode of N-Phenacyldibromobenzimidazoles by Paolo Caliceti, Lukasz Kuryk, Aleksander Gryciuk, Joanna Kawalec, Marta Rogalska, Joanna Baran, Anna Kowalkowska.

Our study aimed to characterise the action mode of N-phenacyldibromobenzimidazoles against C. albicans and neoformans. Firstly, we selected non-cytotoxic most active benzimidazoles based on structure–activity relationships showing that group 5,6-dibromobenzimidazole derivatives are less vs. 4,6-dibromobenzimidazole analogues (5e–f 5h). The substitution chlorine atoms benzene ring N-phenacyl substituent extended anti-C. (5e with 2,4-Cl2 or 5f 3,4-Cl2). excellent results for N-phenacyldibromobenzimidazole 5h reference clinical isolate showed IC50 = 8 µg/mL %I 100 ± 3, respectively. Compound was fungicidal neoformans isolate. at 160–4 caused irreversible damage fungal cell membrane accidental death (ACD). We reported chitinolytic activity 5h, in accordance patterns observed following substrates: 4-nitrophenyl-N-acetyl-β-d-glucosaminide 4-nitrophenyl-β-d-N,N′,N″-triacetylchitothiose. Derivative 16 µg/mL: (1) it affected wall by inducing β-d-glucanase, (2) morphological distortions (3) osmotic instability biofilm-treated. exerted Candida-dependent inhibition virulence factors.

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