Partially retro-inverted tuftsin analogues, method for the...

C - Chemistry – Metallurgy – 07 – K

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530/1, 530/5.06,

C07K 5/06 (2006.01) C07C 271/22 (2006.01) C07K 1/00 (2006.01) C07K 5/02 (2006.01)

Patent

CA 1318457

ABSTRACT OF THE DISCLOSURE: New partially retro-inverted tuftsin analogues of general formula Image wherein R represents the side-chain of the amino acids threonine, methionine or leucine, R1 represents the side- chain of the amino acids lysine or arginine, R2 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 share the pharmacological properties of tuftsin that is stimulating phagocytosis, antibacterial activity of the macrophages and has potential as an immunostimulating, antibacterial and antitumor drug, are more stable toward the enzymatic degradation than the parent molecule.

541628

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