| 摘要 |
FIELD: chemistry of peptides. SUBSTANCE: polypeptides involving peptide of the formula: X-A-A-Trp-Ala-Val-Gly-His-Leu-psi-A-Q where X - hydrogen; simple bond binding alpha-aminogroup of Awith gamma-carboxyl part on 3-propionyl part of Aif Ais Glu; or group of the formula RCO- where Ris taken from the group involving: a) hydrogen, C-alkyl, phenyl or phenyl-C-alkyl, p-HI-phenyl, p-HI-phenyl-C, alkyl, naphthyl, naphthyl-C-alkyl, thienyl, thienyl-C-alkyl, cyclohexyl or cyclohexyl-C-alkyl where HI - F, Cl, Br, OH, CHor OCH; b) N(R)(R) where R- hydrogen, C-alkyl, phenyl or phenyl-C-alkyl and Ris hydrogen or C-alkyl; c) RO- where Ris C-alkyl, phenyl or phenyl-C-alkyl; Ais D- or L-amino acid residue taken from the group: Phe, p-HI-Phe, pGlu, NaI, Pal, Tpi, unsubstituted Trp or Trp substituted at benzene ring with one or some substituents taken from the group: F, Cl, Br, NHor C-alkyl; or Ais peptide bond binding acyl-group of RCO with alpha-amino moiety of Aif Ais Gln, Glu[-], Gly (V) or His where [-] is simple bond binding gamma-carboxyl-group of Awith alpha-aminogroup of Aif Ais Glu where X - simple bond, Y - ORor -N(R)(R) where R- hydrogen, C-alkyl or phenyl; R- hydrogen or C-alkyl; R- hydrogen, C--alkyl or -NHCONH; Leu-psi is reduced form of Leu where C=O part is presented instead -CH- and therefore bind of indicated CH--part with alpha-aminogroup of adjacent A-residue is pseudopeptide bond; A- Tac, MTac or DMTac; and Q - A, NHor OQwhere Qis hydrogen, C-alkyl, phenyl or phenyl-C-alkyl, and pharmaceutically acceptable acids or salts. EFFECT: improved method of synthesis and treatment. |
