| 摘要 |
Cyclic peptides (I), containing 8 amino acid residues and optionally further alpha ,omega -aminocarboxylic acid residues, are new. Cyclic peptides of formula Cyclo-(Arg-X 1-Asp-X 1-X 2-X 3-X 4-X 5-X 6-R 1) (I) and their salts and solvates are new. X 1Ser, Gly or Thr; X 2Leu, Ile, Nle, Val or Phe; X 3Asp, Glu, Lys or Phe; X 4Gly, Ala or Ser; X 5Leu, Ile, Nle, Val or Phe; X 6Arg, Har or Lys; R 1one or more omega -aminocarboxylic acid residues, having a length of 50-2500 mu m; or is absent; the amino acid residues are optionally derivatized and include D- as well as L-forms (in the case of optically active aminoacids). ACTIVITY : Antithrombotic; Cardiant; Antiarteriosclerotic; Cytostatic; Osteopathic; Antiinflammatory; Antibacterial; Antipsoriatic; Vulnerary; Cerebroprotective; Antianginal; Antidiabetic; Ophthalmological; Antiarthritic; Antirheumatic; Antiulcer; Vasotropic; Nephrotropic; Neuroprotective. MECHANISM OF ACTION : alpha vbeta 6-Integrin receptor inhibitor. Cyclo-(Arg-Thr-Asp-Leu-D-Asp-Ala-Leu-Arg-Abu-Abu) (Ia), Abu : 4-aminobutyric acid had IC 500.03 times that of the standard compound Ac-Arg-Thr-Asp-Leu-Asp-Ser-Leu-Arg-NH 2(i.e. 75 nM) in an alpha vbeta 6/fibronectin receptor binding assay. |
