SOMATOSTATIN AGONISTS Russian patent published in 2005 - IPC

FIELD: bioorganic chemistry.

SUBSTANCE: invention provides somatostatin agonists of general formula: A¹-cyclo{Cys-A²-D-Trp-A³-A⁴-Cys}-A⁵-Y¹ (I), wherein A¹ represents aromatic D- or L-α-amino acid selected from Phe, D-Phe, Tyr, D-Tyr, β-Nal, D-β-Nal, Cha, or D-Cha; A² aromatic α-amino acid selected from Phe, Tyr, β-Nal, and Cha; A³ Lys or Orn; A⁴ β-hydroxyvaline, Ser, hSer, or Thr; A⁵ β-hydroxyvaline, Ser, hSer, or Thr; and Y¹ represents NH₂; amide nitrogen atoms of peptide groups and amine group of A¹ in compound I are optionally substituted by methyl group, provided that at least one methyl group is available and that compound I cannot have following formula: D-Phe-cyclo{Cys-Phe-D-Trp-Lys-(N-Me-Thr)-Cys}-Thr-NH-₂. pharmaceutically acceptable salts of compound I are also claimed.

EFFECT: expanded synthetic possibilities in peptide synthesis.

24 cl, 2 tbl, 18 ex