Bradykinin antagonists modified with dipeptide mimetic β-turn inducers

Bradykinin (BK) is involved in a wide variety of pathophysiological processes. Potent BK peptide antagonists can be developed introducing constrained unnatural amino acids, necessary to force the secondary structure of the molecule. In this paper, we report a structure–activity relationship study of two peptide analogues of the potent B2 antagonist HOE 140 by replacing the D-Tic-Oic dipeptide with conformationally constrained dipeptide mimetic β-turn inducers.

Graphical abstractA structure–activity relationship study of Icatibant analogues modified with dipeptide mimetic β-turn inducers is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide