The exploration of food-derived bioactive compounds offers unprecedented opportunities for drug discovery and therapeutic innovation. Beyond their nutritional role, foods contain a wealth of chemically diverse molecules capable of modulating critical biological pathways involved in infection, inflammation, neurodegeneration, and cancer. Foodomics approaches, including metabolomics and multi-omics analyses, now allow the systematic identification, characterization, and functional assessment of these bioactive compounds, providing a bridge between natural product discovery and medicinal chemistry.

Translating food-derived compounds - such as polyphenols, terpenoids, peptides, and lipids - into effective therapeutics requires overcoming challenges related to bioavailability, stability, and target specificity. Advanced drug delivery systems play a pivotal role in enhancing solubility, stability, and tissue-specific targeting, enabling optimized pharmacokinetic and pharmacodynamic profiles.

This Special Issue, “Food-Derived Bioactive Compounds: From Foodomics to Therapeutic Applications,” invites contributions - original articles and reviews - on all aspects of the medicinal chemistry–driven development of food-derived molecules. Topics of interest include lead discovery, chemical optimization, structure–activity relationships, delivery strategies, and translational applications, particularly in antimicrobial, neuroprotective, and anticancer contexts. By combining foodomics, medicinal chemistry, and pharmaceutical technology, this Special Issue aims to highlight innovative strategies that unlock the therapeutic potential of bioactive compounds from foods.

Keywords: Food-derived bioactive compounds, foodomics, metabolomics and multi-omics approaches, functional foods and nutraceuticals, bioactive metabolites, drug discovery from natural products, antimicrobial compounds, neuroprotective agents, anticancer compounds, advanced drug delivery systems