Abstract: The present study describes the synthesis of some novel analogues (I-IV) of an anti-inflammatory peptide-based drug called Oxpholipin-11 D. Chemical modifications in the peptide chain sequences were introduced to the parent compound, aiming to enhance the potency and penetration properties of the resulting peptide analogues. These novel compounds were characterized by means of their amino acid analysis, FT-IR and HPLC-ESI-mass spectra. The biological evaluation of the obtained compounds showed increased anti-inflammatory activity of the analogues I, II and IV compared to the reference drug.