SYNTHESIS OF NONPEPTIDE BRADYKININ B-2 RECEPTOR ANTAGONISTS

The syntheses of the potent, competitive bradykinin B-2 receptor antag onists, 1-3, are described. These compounds represent the three struct ural classes of B-2 receptor antagonists discovered in our program. Co mpounds 1-3 bind to the human IMR 90 fetal lung fibroblast bradykinin B-2 receptor with affinity constants K-i = 3.4 mu M, 0.77 mu M, and 0. 060 mu M, respectively.