Antimicrobial and antibiofilm activity of iodo(telluro)-induced heterocyclization products of terminal 2-alkynylthioquinoline-3-carbaldehydes
Abstract
Antimicrobial resistance represents a major global public health challenge, causing increased morbidity and mortality from i n fectious diseases and imposing substantial economic burdens on healthcare systems worldwide. O ur objective was to evaluate the activity of newly synthesized tellurium- and halogen-functionalized quinoline derivatives against planktonic and biofilm forms of opportunistic microorganisms. The antimicrobial activity of the newly synthesized compounds was evaluated using the broth microdilution method against clinical isolates of Staphylococcus aureus , Candida albicans , Escherichia coli , and Enterococcus faecalis . Compounds demonstrating the highest antimicrobial activity were subsequently assessed for antibiofilm efficacy using the 96-well microtiter plate assay. The most pronounced antimicrobial activity was demonstrated by 1-iodomethylidene-5-formyl-2,3-dihydro[1,3]thiazino[3,2-a]quinolinium bromide (4), the complex 1-{[dichloro(4-methoxyphenyl)-λ⁴-tellanyl]methylidene}-5-formyl-2,3-dihydro[1,3]thiazino[3,2-a]quinolinium chloride with 4-methoxyphenyltellurium trichloride (6), 1-iodomethylidene-4-formyl-1,2-dihydro[1,3]thiazolo[3,2-a]quinolinium chloride (2), and 1-(dichloro-λ⁴-tellanylmethylidene)-5-formyl-2,3-dihyd ro[1,3]thiazi no[3,2-a]quinolinium bromide (10). These compounds were therefore selected for evaluation of their antibiofilm pro p erties. Compounds 2 and 10 exhibited the strongest antibiofilm activity, completely disrupting established biofilms formed by the tested microbial strains. By contrast, compound 4 demonstrated enhanced antibiofilm efficacy at higher dilutions (lower concentr a tions). A similar concentration-dependent pattern was observed for compound 6 against E. faecalis biofilms. Novel tellurium- and halogen-functionalized quinoline derivatives demonstrated pronounced antimicrobial and antibiofilm activity against clinical is o lates of opportunistic microorganisms. The strongest inhibitory effects were observed against the microscopic fungus Candida albicans . These findings highlight the investigated compounds as promising candidates for further development as antiseptic and disinfectant agents to control infections, including biofilm-associated and healthcare-related infections.References
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