Phenolamides constitute a family of metabolites, widely represented in the plant kingdom, that can be found in all plant organs with a predominance in flowers and pollen grains. They represent a large and structurally diverse family, resulting from the association of phenolic acids with aliphatic or aromatic amines. Initially revealed as active compounds in several medicinal plant extracts, phenolamides have been extensively studied for their health-promoting and pharmacological properties. Indeed, phenolamides have been shown to exhibit antioxidant, anti-inflammatory, anti-cancer and antimicrobial properties, but also protective effects against metabolic syndrome and neurodegenerative diseases. The purpose of this review is to summarise this large body of literature, including in vitro and in vivo studies, by describing the diversity of their biological properties and our actual knowledge of the molecular mechanisms behind them. With regard to their considerable pharmacological interest, the question of industrial production is also tackled through chemical and biological syntheses in engineered microorganisms. The diversity of biological activities already described, together with the active discovery of the broad structural diversity of this metabolite family, make phenolamides a promising source of new active compounds on which future studies should be focused.