Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines

A series of 2-[(heteroaryl)methyl]imidazolines was synthesized and tested for their activities at α1- and α2-adrenoceptors and imidazoline I1 and I2 receptors. The most active 2-[(indazol-1-yl)methyl]imidazolines showed high or moderate affinities for α1- and α2-adrenoceptors. However, their intrinsic activities at α2A-adrenoceptors proved to be negligible. A selected 7-chloro derivative behaved as a potent α1-adrenoceptor antagonist and exhibited peripherally mediated hypotensive effects in rats.