Novel heterocycles as selective α1-adrenergic receptor antagonists

A novel series of aryl piperazine substituted heterocycles has been synthesized and identified as antagonists of the α1a-adrenergic receptor (α1a-AR), which has been implicated in benign prostatic hyperplasia (BPH). These compounds selectively inhibit binding to the α1a-AR with Kis as low as 2.1 nM.