5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists

A series of 2,3-diaminopyridine bradykinin B1 antagonists was modified to mitigate the potential for bioactivation. Removal of the 3-amino group and incorporation of basic 5-piperazinyl carboxamides at the pyridine 5-position provided compounds with high affinity for the human B1 receptor.

A series of 2,3-diaminopyridine bradykinin B1 antagonists was modified to mitigate the potential for bioactivation. Removal of the 3-amino group and incorporation of basic 5-piperazinyl carboxamides at the pyridine 5-position provided compounds with high affinity for the human B1 receptor.Figure optionsDownload as PowerPoint slide