The present invention relates to a serine derivative compound having improved blood-brain barrier (BBB) permeability and the use thereof, and more particularly, to a novel serine derivative compound having improved blood-brain barrier permeability compared to L-serine, and a pharmaceutical composition for preventing, treating or alleviating nervous system diseases such as cognitive disorder, intellectual disability, microcephaly, epilepsy, neurodevelopmental disorder, dementia, autism spectrum disorder, Down's syndrome, Rett's syndrome, fragile X syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis, the pharmaceutical composition containing the compound as an active ingredient. The compound of Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient for the pharmaceutical composition for preventing or treating central nervous system diseases according to the present invention exhibits significantly improved blood-brain barrier permeability, activates neuronal cell proliferation, and exhibits a neuronal protective effect of inhibiting neuronal cell death resulting from mitochondrial membrane potential damage and/or endoplasmic reticulum stress caused by oxidative stress, and exhibits improved blood-brain barrier permeability. Therefore, the compound has an excellent effect on the prevention, treatment and alleviation of central nervous system diseases such as cognitive disorder, intellectual disability, microcephaly, epilepsy, neurodevelopmental disorder, dementia, autism spectrum disorder, Down's syndrome, Rett's syndrome, fragile X syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis, and thus is a highly useful invention in the pharmaceutical industry, the food industry and the livestock industry.