The invention relates to chiral pyrazolone spiro [ethylenethiourea] spirooxindole compounds and derivatives thereof. The chiral pyrazolone spiro [ethylenethiourea] spirooxindole compounds and the derivatives thereof have structures shown in general formulae II and III, wherein R<1> and R<2> are independently selected from C1-6 alkyl, phenyl, substituted phenyl, benzyl, phenethyl, phenylpropyl, thienyl and naphthyl respectively; R<3> is selected from hydrogen, C1-6 alkyl, C1-6 alkenyl and benzyl; R<4> is selected from hydrogen, C1-6 alkyl, phenyl, halogen, C1-6 alkoxy and C1-6 halogenated alkyl; R<5> is selected from hydrogen, carbalkoxy, acetyl and phenyl. The compounds are prepared from 4-position non-substituted pyrazolone through a synthetic reaction. A series of hCE1 (human carboxylesterase 1) inhibitors are developed on the basis of pyrazolone spiro [ethylenethiourea] spirooxindole skeletons, so that potential selections are provided for treatment of hCE1 related diseases such as hyperlipidemia and the like.