Investigation of the EtOAc fraction of Tagetes minuta L. (Asteraceae) aerial parts has afforded a new flavonol glucoside, minutaside A (quercetagetin 6‐O‐(6‐O‐hexanoyl)‐β‐D‐glucopyranoside) (1), together with four known flavonoids: axillarin 7‐O‐β‐D‐glucopyranoside (2), quercetagetin 3,7‐dimethoxy‐6‐O‐β‐D‐glucopyranoside (3), quercetagetin 7‐methoxy‐6‐O‐β‐D‐glucopyranoside (4), and quercetagetin 6‐O‐β‐D‐glucopyranoside (5). Their structures were established by multiple spectroscopic methods in addition to HRESIMS (high‐resolution electrospray ionisation mass spectra) and comparison with literature data. The antioxidant and anti‐diabetic activities of the isolated flavonoids were evaluated using 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and α‐amylase inhibition assays. Compounds 1 and 5 showed significant antioxidant activity (84.1 and 83.0% at a 20 μM dose, respectively). Compounds 1, 4, and 5 exhibited strong α‐amylase inhibitory activity compared with acarbose (a reference α‐amylase inhibitor). However, 2 and 3 showed moderate activity. Molecular modeling studies of 1–5 that included docking, flexible alignment, and surface mapping were performed to evaluate their recognition profile α‐amylase receptor. In docking simulations, 5 displayed a binding mode similar to that of acarbose in the active site of α‐amylase enzyme.