Sulfonamido-aryl ethers as bradykinin B1 receptor antagonists

The synthesis and identification of sulfonamido-aryl ethers as potent bradykinin B1 receptor antagonists from a ∼60,000 member encoded combinatorial library are reported. Two distinct series of compounds exhibiting different structure–activity relationships were identified in a bradykinin B1 whole-cell receptor-binding assay. Specific examples exhibit Ki values of ∼10 nM.

Graphical abstractTwo distinct series of sulfonamido-aryl ethers as potent bradykinin B1 receptor antagonists consistent with a proposed B1 antagonist pharmacophore are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide