| 摘要 |
<p>Amino acid cyclic amide derivatives (I) are new. Amino acid cyclic amide derivatives of formula (I) are new. B-A-C (I) A : an alpha -amino acid with a side-chain functional group; B : a molecule covalently bonded to the side-chain functional group of A, selected from oligopeptides with a chain length of up to 20 amino acids, polyethylene glycol (PEG) with a molecular weight of up to 20,000, optionally substituted organic amines, amides, alcohols, acids or aromatics with 8-50 C atoms; C : a thiazolidine (Thia), pyrrolidine, hydroxyproline, dehydroproline or piperidine group forming an amide bond with A. ACTIVITY : Antiinflammatory; antiallergic; dermatological; antiarthritic; antipsoriatic; immunomodulator; cytostatic. MECHANISM OF ACTION : Dipeptidyl peptidase IV (DP IV) modulator. The serum DP IV activity of rats after oral administration of 5 mu M Glu(PEG)-Thia was increased by almost 10% after 20 minutes and then decreased to 90% of the initial level over the next 100 minutes.</p> |
