Partially retro-inverted tuftsin analogues, method for the preparation thereof and pharmaceutical compositions containing them.

摘要

New partially retro-inverted tuftsin analogues of general formula I <CHEM> wherein R represents the side-chain of the amino acids threonine, methionine or leucine R<1> represents the side-chain of the amino acids lysine or arginine R<2> is hydrogen or a metabolically labile acyl group, all the asymmetric carbon atoms are either of the S- or R-configuration, or, alternatively, the first, third, and fourth asymmetric carbons, starting from the N-terminal residue, are of the S-configuration while the second one is of the R- or (R,S)-configuration, and the corresponding pharmacologically acceptable salts, esters and amides. The new compounds which share the same pharmacological properties of tuftsin, are much more stable toward the enzymatic degradation than the parent molecule.