The invention relates to an N-substituted
pipecolic acid derivative or a pharmaceutically acceptable salt thereof which is represented by the general formula (I) in the specification, wherein A1 represents H and straight-chained or
branch-chained
alkyl or benzyl of C1-4, and A2 represents amino, straight-chained or
branch-chained
alkyl amino of C1-4, straight-chained or
branch-chained dialkyl amino of C1-4 and 5-7 membered heterocyclic amino containing 1-2 heteroatoms of N, O or S; and the premise condition is that a heterocyclic ring contains an N
heteroatom connected with a mother
nucleus of the general formula (I). The invention further relates to a preparation method of the N-substituted
pipecolic acid derivative, a pharmaceutical composition which has potential application values in treatment of neurodegenerative diseases and effects of regenerating and protecting neurons, and an application in preparation of pharmaceutical preparations which are favorable for improving the functions of a
nervous system, including the treatment of
brain dysfunction, neurodegenerative diseases and
functional disorder diseases caused by insufficient cerebral
blood supply or
neurotransmitter deficiency.