Document Report Card
Basic Information
ID: ALA1141596
Journal: Bioorg Med Chem Lett
Title: A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.
Authors: Feng DM, DiPardo RM, Wai JM, Chang RK, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG, Kuduk SD.
Abstract: The design and synthesis of a novel class of human bradykinin B1 antagonists featuring difluoroethyl ether and isoxazole carboxamide moieties are disclosed. Compound 7g displayed excellent pharmacokinetic properties, efficient ex vivo receptor occupancy, and low potential for P450 induction via PXR activation.
CiteXplore: 18240388