Novel small molecule bradykinin B1 receptor antagonists. Part 3: Hydroxyurea derivatives
Hydroxy urea moieties are introduced as a new class of bradykinin B1 receptor antagonists. First, the SAR of the lead compound was systematically explored. Subsequent optimization resulted in the identification of several biaryl-based hydroxyurea bradykinin B1 receptor antagonists with low-nanomolar activity and very high oral bioavailability in the rat.