The Antifungal Action Mode of -Phenacyldibromobenzimidazoles.

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