Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands

A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor. Structure–activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H4 receptor.

A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor.Figure optionsDownload as PowerPoint slide