Oxyprenyl-chalcones as antibacterial hits: design of experiments-optimized synthesis, antibacterial evaluation, early drug-like profiling and biodegradability prediction.

ABSTRACT: The escalating threat of antimicrobial resistance (AMR) compels the development of novel antibiotics with broad spectrum activity and environmentally responsible degradation profiles. Chalcones, naturally occurring 1,3-diaryl-2-propen-1-ones, have emerged as promising scaffolds due to their pleiotropic bioactivity and structural tunability. In this study, we explored the synthesis and functionalization of oxyprenylated chalcones as potential antibacterial compounds and explored their functionalization with protonatable moieties to enhance their affinity for bacterial membranes and their solubility properties. Starting from hydroxycordoin 1a, we synthesized a series of isomeric and hydroxy derivatives, with the aim of studying their structure-activity relationships, and based on the initial

SUBMITTER: Marotta L 

PROVIDER: S-EPMC12863399 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature