To study the chemical constituents from the aerial parts of Scoparia dulcis. Various chromatographic techniques were used to separate the constituents and their structures were elucidated using spectroscopic methods and by comparing their data to those reported in the literatures. The α-glucosidase inhibitory activity assay was used to identify potential α-glucosidase inhibitors. Nine compounds were isolated from the aerial parts of S. dulcis. Their structures were identified as Scoparic zolone (1), (2S)-2,7-dihydroxy-2H-1,4-benzoxazin-3(4H)-one (2), (2R)-7-hydroxy-2H-1,4-benzoxazin-3(4H)-one-2-O-β-d-glucopyranoside (3), (2R)-7-methoxy-2H-1,4-benzoxazin-3(4H)-one-2-O-β-d-glucopyranoside (4), (2S)-7-hydroxy-2H-1,4-benzoxazin-3(4H)-one-2-O-β-d-glucopyranoside (5), 6-methoxy-benzoxazolin-2(3H)-one (6), 4-acetonyl-3,5-dimethoxy-p-quinol (7), zizyvoside I (8), and 3,4-dihydroxy benzeneacetic acid (9). Compound 2 showed the potent α-glucosidase inhibitory activity with an IC50 value of (132.8 ± 11.5) μmol/L, which is 28-fold higher than the positive control acarbose. Compound 1 is a new natural product. Compounds 2 and 9 have not been reported in Scoparia before. Compounds 3, 5, 7, 8 are isolated from Scrophulariaceae for the first time.