SMALL MOLECULE OF INHIBITORS OF ENZYMATIC ACTIVITY OF ROTAMASE Russian patent published in 2002 - IPC

FIELD: organic chemistry, biochemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel neurotropic derivatives of N-glyoxylpropyl ester of the formula (I): where R₁ means C₁-C₅-alkyl with direct or branched chain possibly substituted with C₃-C₆-cycloalkyl, C₃-, C₅-, C₆-cycloalkyl or Ar₁ where Ar₁ is taken among the group including 2-thienyl, 2-furanyl, 2-thiazolyl or phenyl; X means oxygen atom; Y means oxygen atom or NR₂, where R₂ means hydrogen atom; Z means C₂-C₆-alkyl or alkenyl with direct or branched chain that is substituted by one or more positions with Ar₂ or C₃-C₆-cycloalkyl where Ar₂ is taken among the group including phenyl, 2-, 3- or 4-pyridyl, phenyl, substituted methylenedioxy-group and phenyl comprising from one to three substituents which mean independently chlorine atom or C₁-C₄-alkoxy-group, or its pharmaceutically acceptable salts or hydrates. Compounds of the formula (I) show affinity to proteins binding FK-506, for example, FKBP-12. They inhibit activity of proline-peptidyl-cis, trans-isomerase or rotamase of binding protein and stimulate growth of axons and show the absence of immunosuppressive effect that ensures to use their in treatment of neurological diseases or in cases when the stimulation of regeneration and growth of nerves is desirable. EFFECT: valuable medicinal properties. 11 cl, 26 dwg, 2 tbl, 30 ex