Effects of white sorghum brewing process on free amino-acids, c-aminobutyric acid (GABA), phenolics and bioactivity, including antioxidant (by ABTS + and reducing power, RP, methods), antihypertensive (angiotensin converting enzyme-I, ACE-I inhibition assay), and hypoglycaemic activity (a-glucosidase inhibition assay) were evaluated. From the wort to the beer, free amino acids decreased, but GABA and phenolics increased significantly, positively modifying the bioactive potential. ABTS and a-glucosidase inhibition activity correlated positively with at least one of the phenolic acids evaluated. Ale white sorghum beer presented high content of GABA (7.8 mg L À1 ), phenolics (40.7 mg total phenolic acids L À1 ), antioxidant activity (9.14 mmol Trolox equivalent L À1 , and 48.8 mmol ascorbic acid equivalent L À1 , for ABTS + and RP, respectively), and exhibit ACE-I inhibition (1.0 lg captopril equivalent L À1 ) and a-glucosidase inhibition (34.5 mg acarbose equivalent L À1 ) activities. The level of bioactive compounds and its low ethanol content (2.3%), make beer obtained from malted white sorghum a potential functional beverage.