Phenyl‐oxazoles, a New Family of Inverse Agonists at the H₃ Histamine Receptor

Drug design: Oxazoles and thiazoles were designed and synthesised based on previously reported ligands of the 3rd histamine receptor (H3R). The aminopropoxy-phenyl-oxazole chemotype was identified as a promising H3R inverse agonist with superior drug-like properties, good efficacy in vivo and good safety margin.