Click-based synthesis of bromotyrosine alkaloid analogs as potential anti-biofilm leads for SAR studies.

A library of triazole-based analogs of bromotyramine alkaloids such as verongamines, hemibastadins, pseudoceramine D and clavatidine E was designed in order to identify promising leads that may help in the control of bacterial biofilms. Twenty-three compounds were screened for their biofilm inhibitory activity against three strains of Gram-negative bacteria. SAR studies revealed that hemibastadins analogs were the most active compounds which act as inhibitors of biofilm development (EC50 8.8-29μM) without effect on bacterial growth even at high concentrations (100μM).