This spotlight on application provides a brief overview of our research exploration, focusing on the research of small molecules with membrane-active antibacterial activity that mimic host-defense peptides (HDPs). The development of antimicrobial HDP agents is an emerging research area as they circumvent the potential disadvantages of HDPs. The small molecules are preferable for development due to their low production cost and potential of more practical applications. In recent years, we conducted research on the design of antibacterial agents based on small molecules including hydantoins, acylated reduced amides, biscyclic guanidines, and dimeric alkylamides of lysines. We herein sketch our journey on the exploration of the antimicrobial activity of these few classes of molecules and hopefully share our insight in the future design of small-molecular-weight antibiotic agents with membrane-active activity that mimic HDPs.
Keywords: Antibacterial; Antibiotic resistance; HDPs; Membrane activity; Small molecules.