Author:

Abstract:

Nowadays, biofilms are considered as an important factor in multiple medicinal and industrial issues. They have a profound resistance against antibiotics and disinfectants, which makes it nearly impossible to eradicate them. Therefore, during the last decade, many efforts in the development of biofilm preventing molecules have been made. Out of the investigated compounds, the 2-aminoimidazoles (2AI) have showed promising biofilm specific activity. The first chapter of this thesis is dedicated to the further extension of the 2-aminoimidazole scaffold. A novel substituent pattern was proposed based on the merger of the substituent pattern of previously developed 2-AI compound classes. The novel class was found to possess biofilm-specific activity against biofilm formation of Gram-positive bacteria. The second chapter is dedicated to the development of biofilm inhibiting surfaces. Prosthetics and implants can serve as an ideal surface for biofilm formation after surgery. Biofilm inhibiting surfaces could serve as a solution. As a proof of concept, aminomethylated polystyrene lanterns were functionalised with 2-AIs. Biofilm inhibition was observed but due to the shape of the lanterns a quantification was complicated. Therefore, Ti-surfaces were functionalised with the most potent 2-AI developed. The Ti-implants were found to have good in vitro and in vivo activity against biofilm formation of Staphylococcus aureus and increased the growth of bone cells. The final chapter describes the synthesis and activity of novel 2-AI analogues. A late stage modification approach towards 2-substituted imidazole was developed. From the synthesized scaffolds, 2-methaminomidazole possessed the most promising activity against biofilm formation of Salmonella typhymirium.