| 摘要 |
PURPOSE: A cyclic peptide analog of somatostatin or pharmaceutically acceptable salt thereof is provided which can be used to inhibit the release of insulin in a mammal such as a human patient. CONSTITUTION: A cyclic peptide analog of somatostatin, wherein a disulfide bond links the N-terminus residue and the C-terminus residue, has the structure of the formula, in which: A1 is the D- or L- isomer of Cys or Mpa; A2 is Asn, Gln, an aliphatic amino acid, an aromatic amino acid or deleted; A3 is an aromatic amino acid; A4 is His or an aromatic amino acid; A7 is Thr, Ser or an aliphatic amino acid; A8 is an aromatic amino acid; A9 is the D- or L- isomer of Cys; each of R1 and R2 is independently H, C1-12 alkyl, C7-20 hydroxyphenylalkyl, C11-20 naphthylalkyl, or COE1 where E1 is C1-12 alkyl, C7-20 phenylalkyl, C11-20 naphthylalkyl, C1-12 hydroxyalkyl, C7-20 hydroxyphenylalkyl, or C11-20 hydroxynaphthylalkyl; and R3 is NH2 or NHYCH2Z wherein Y is a C1-12 hydrocarbonmoiety and Z is H, OH, CO2H or CONH2; and disulfide bond links the side chain of residue A1 and A9.
|
