Stephen A. Munk

Analogs of UK 14,304: Structural features responsible for α2 adrenoceptor activity

Abstract Factors influencing the potency of UK 14,304 analogs including conformational preorganization and arrangement of hydrogen bond acceptors on the aromatic core are described. The previously reported importance of twist of the iminoimidazoline ring relative to the core for enhanced α 2 activity is supported.

Analogs of UK 14,304 as α2-adrenoceptor agonists. Twist and agent polarity as design elements

Abstract Tetrahydroquinoxaline analogs of UK 14,304 were prepared. These agents proved to be highly polar, potent, and selective α 2 -adrenoceptor agonists. This study suggested that agents bearing a twist of the imidazoline ring relative to the quinoxaline nucleus prove more potent than planar analogs.