Wheatgrass and barley grass are freshly sprouted leaves of wheat and barley seeds and are rich sources of phytochemicals. This study was conducted to investigate the effects of drought stress on the biochemical compounds and antioxidant activities of barley grass and wheatgrass extracts. The grass was cultivated in an organic soil growing medium with different levels of drought stress (a control with 100% water holding capacity (WHC), mild drought stress with 75% WHC, moderate drought stress with 50% WHC, and severe drought stress with 25% WHC) in a growth chamber by controlling temperature (20/15 °C, day/ night), light (12/12 h, light/dark; intensity 150 ∼mol m −2 s −1 with quantum dot light-emitting diodes), and relative humidity (60%) for 7 days. The drought stress showed increased levels of biochemical compounds, especially phenolics, flavonoids, and vitamin C, in both barley grass and wheatgrass extracts. The wheatgrass extracts showed 1.38-1.67 times higher phenolics, flavonoids, and vitamin C contents than the barley grass extracts did. The antioxidant (2,2 0 -azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activity, and nitrite-scavenging activity) and antioxidant enzymes (guaiacol peroxidase, catalase, and glutathione reductase) were the highest under severe drought stress in both barley grass and wheatgrass extracts; and the wheatgrass extracts showed 1.20-5.70 times higher antioxidant enzyme activities than the barley grass extracts did. Proper drought-stress treatment of barley grass and wheatgrass may be a convenient and efficient method to increase biochemical compounds and antioxidants in our diet to exploit the related health benefits.