FIELD: organic chemistry. SUBSTANCE: product: derivatives of hydrazine of the general formula (I): R1R2N-C(R3R4)-C(R5R6)-N-(R7)-N-(R8R9) (I) where: R1 and R9 mean independently - hydrogen, lower alkanoyl, phenyl-(lower)-alkanoyl, phenyl-(lower)-alkanoyl where residue of lower alkanoyl is substituted with carbamoyl, morpholino-(lower)-alkanoyl, thiomorpholino-(lower)-alkanoyl, pyridyl-(lower)-alkanoyl, quinolyl-(lower)-alkanoyl, tetrazolyl-(lower)-alkanoyl, amino-(lower)-alkanoyl substituted at amine nitrogen with N-morpholino- or N-thiomorpholinocarbonyl, halogen-(lower)-alkanoyl containing up to three halogen atoms, 2-(morpholino-(lower)-alkylcarbamoyl)-lower alkanoyl, 2-(N-pyridyl-(lower)-alkylcarbamoyl)-lower alkanoyl, lower alkoxycarbonyl, phenyl-(lower)-alkoxycarbonyl, tetrahydrofuranyl-(lower)-alkylhydroxycarbonyl, lower alkylsulfonyl, N-pyridyl-(lower)-alkyl-N-(lower)-alkylcarbamoyl, or amino acid acyl residue taken from: glycine, alanine, valine, leucine, isoleucine, glutamic acid and asparagine in the form of (D)-, (L)- or (D,L)-isomers where α-amino group is free or acylated with one of above indicated residue R1 or R9 at condition that at least one of residue R1 and R9 means hydrogen; R2, R4, R6 and R8 mean hydrogen; R3 - lower alkyl, cyclohexyl-(lower)-alkyl or phenyl-(lower)-alkyl that can be free or substituted with halogen lower alkoxy or cyano-groups; R5 means hydroxyl group; R7 - lower alkyl, cyclohexyl-(lower)-alkyl or phenyl-(lower)-alkyl that can be free or substituted with halogen, lower alkoxy or cyano-groups, or their salts. Pharmaceutical agent has an effective dose of compounds of the formula (I) and hydrazine derivative of the formula (II) H2N-HC(R3)-CH-(OH)-N-(R7)NH2 (II) - intermediate compounds for synthesis of (I). Synthesized compounds inhibit activity of enzyme protease and show antiviral activity. EFFECT: improved method of synthesis. 10 cl
Authors
Dates
1997-10-10—Published
1992-07-02—Filed