Bradykinin B1 antagonists: Biphenyl SAR studies in the cyclopropanecarboxamide series

SAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B1 antagonists was examined. Incorporation of a pyridine in place of the proximal phenyl ring and chlorination of the distal phenyl ring proved to be well tolerated and provided compounds with improved pharmacokinetic profiles, CNS penetration, and enhanced receptor occupancy.

SAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B1 antagonists was examined.Figure optionsDownload as PowerPoint slide