PSEUDOPENTAPEPTIDES WITH IMMUNOMODULATING ACTIVITY

摘要

Pseudopeptides of formula ( alpha ) wherein AA1 is an arginyl residue; AA2 is a basic amino acid residue, a neutral/nonaromatic amino acid residue or proline residue or is an N-alkylated (1-6C) form thereof; AA3 is an aspartic acid or glutamic acid wherein the remaining carboxyl group may be esterified with alkyl (1-6C), or an alanine residue; AA4 is a neutral/nonaromatic amino acid residue; AA5 is a neutral/aromatic amino acid residue wherein one or more hydrogens of its aromatic portion can be substituted by NO2 or halogen, or is a neutral/nonpolar/large/nonaromatic amino acid residue or the N-alkylated (1-6C) form thereof; R is acyl (1-6C), arylsulfonyl, alkylsulfonyl, arylalkylsulfonyl or alkoxycarbonyl group; and R1 is -OH, -NR2R3 or -OR4 wherein each of R2 and R3 is hydrogen or an alkyl group (1-6C) and R4 is alkyl group (1-6C); and wherein at least one of the linkages I-IV is a modified peptide linkage -COCH2-, -CH(OH)CH2- or -CH2NH-, and the remaining linkages are -CONH- or -CON(CH3)-.