1-Benzylbenzimidazoles: The discovery of a novel series of bradykinin B1 receptor antagonists

The design, synthesis, and structure–activity studies of a novel series of BK B1 receptor antagonists based on a 1-benzylbenzimidazole chemotype are described. A number of compounds, for example, 38g, with excellent affinity for the cynomolgus macaque and rat bradykinin B1 receptor were discovered.

Graphical abstractThe design, synthesis, and structure–activity studies of a novel series of BK B1 receptor antagonists based on a 1-benzylbenzimidazole chemotype are described. A number of compounds, for example, 38g, with excellent affinity for the cynomolgus macaque and rat BK B1 receptor were discovered.Figure optionsDownload full-size imageDownload as PowerPoint slide