Discovery of a series of (4,5-Dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists

A novel (4,5-dihydroimidazol-2-yl)-biphenylamine series of 5-HT7 agonist compounds was developed from a structurally related lead compound 1. The newly discovered series is exemplified by compound 2 that possesses high affinity for 5-HT7 receptors and shows intrinsic agonist activity in functional assays. This new series has significant α1 and α2 activities perhaps due to the presence of the 2-aminoimidazoline moiety.