Biological Assessments of Novel Ultrasound-Synthesized 2-Arylbenzimidazole Derivatives: Antiproliferative and Antibacterial Effects

Abstract

This paper describes ultrasound synthesis, structural characterization and biological activity of new derivatives of 2-arylbenzimidazole 12–27 and 1,2,3-triazole derivatives of 2-arylbenzimidazole 28–33. The tautomeric structures of the prepared target compounds were confirmed by 1H- and 13C-NMR spectroscopy as well as by two-dimensional NOESY, HSQC and HMBC methods. The synthesized compounds underwent in vitro antiproliferative assays, revealing that compound 23 exhibited the highest potency against chronic myeloid leukemia cells (K-562, IC₅₀ = 2.0 μM) and non-Hodgkin's lymphoma cells (Z-138, IC₅₀ = 2.0 μM). Compound 23 was further evaluated for cytotoxicity on normal peripheral blood mononuclear cells (PBMC), and its mechanism of action was investigated. The antibacterial properties of the synthesized compounds were assessed against both Gram-positive and Gram-negative bacterial strains. Derivatives 15–17 exhibited significant selective antibacterial activity against the Gram-positive bacterium Enterococcus faecalis (MIC = 0.25–1 µg mL-1). Additionally, among the 1,2,3-triazole derivatives of 2-arylbenzimidazole, compounds 28 and 30 demonstrated strong selective activity against Enterococcus faecalis (MIC = 0.25 µg mL-1).