Parallel synthesis of a bis-triazoles library as psammaplin A analogues: A new wave of antibiofilm compounds?

Synthesis of psammaplin A analogues is described. Screening for antibiofilm activity of the targeted library afford some interesting elements in terms of structure-activity relationships. Some compounds exhibited EC50 in the range of ampicillin against three strains of gramnegative bacteria without toxic effect.     

Screening of bromotyramine analogues as antifouling compounds against marine bacteria

Rapid and efficient synthesis of 23 analogues inspired by bromotyramine derivatives, marine natural products, by means of CuSO₄-catalysed [3+2] alkyne–azide cycloaddition is described. The final target was then assayed for anti-biofilm activity against three Gram-negative marine bacteria, Pseudoalteromonas ulvae (TC14), Pseudoalteromonas lipolytica (TC8) and Paracoccus sp. (4M6). Most of the synthesised bromotyramine/triazole derivatives are more active than the parent natural products Moloka’iamine (A) and 3,5-dibromo-4-methoxy-β-phenethylamine (B) against biofilm formation by the three bacterial strains. Some of these compounds were shown to act as non-toxic inhibitors of biofilm development with EC₅₀ < 200 μM without any effect on bacterial growth even at high concentrations (200 μM).