γ-aminobutyric acid (GABA) is a natural non-protein amino acid and a significant inhibitory neurotransmitter in the mammalian central nervous system. It plays a vital role in the human cerebral cortex, hippocampus, thalamus, basal ganglia, and cerebellum, and can regulate various body functions. GABA has an essential influence on some pathological conditions caused by the inhibition of nerve activity. When the concentration of GABA in the brain stays low, the nerve impulse is excited and the patient has excessive nerve activity, resulting in anxiety, epilepsy, and other emotions. At present, the small molecule drugs under research can specifically bind to the GABA receptor. The binding enhances the activity of GABAA receptor and weakens the abnormal discharge of brain neurons, which can have wide application in treating anxiety disorders, sleep disorder, and epilepsy. The global patent application for this series of compounds is being submitted.