Disclosed in the present invention are compounds having an aldolase selective inhibiting activity, a preparation method therefor, a pharmaceutical composition comprising the compounds, and uses of the compounds in preparation of drugs for inhibiting synthesis of triglyceride and cholesterol, drugs for reducing synthesis of fatty acid, drugs for preventing and/or treating obesity and II-type diabetes mellitus, drugs for preventing and/or treating tumors, drugs for preventing and/or treating Parkinsonism, drugs for preventing and/or Alzheimer's diseases, or drugs for prolonging the life of mammals.