Bioorg Med Chem Lett. 2021 Jul 10:128259. doi: 10.1016/j.bmcl.2021.128259. Online ahead of print.
Bacterial biofilms often cause medical complications and there has been a great deal of interest in the discovery of small-molecule agents that can inhibit the formation of biofilms. Among these agents, it has been reported that several D-amino acids, such as D-Leu, D-Trp, D-Tyr, and D-Met, exhibit weak inhibitory activity toward bacterial biofilm formation. In this study, we have screened a library of 332 non-proteinogenic amino acids for new biofilm inhibitory agents and discovered several compounds exhibiting biofilm-inhibitory activity against Gram-positive bacteria. In particular, H-DL-β-(3,4-dihydroxyphenyl)-DL-Ser-OH (253) showed potent activity against S. aureus, including methicillin-resistant S. aureus.