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

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