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

  • Bioorg Med Chem. 2012 Jan 1;20(1):108-16. doi: 10.1016/j.bmc.2011.11.025.
Jaroslaw Saczewski  1 ,  Alan Hudson ,  Mika Scheinin ,  Apolonia Rybczynska ,  Daqing Ma ,  Franciszek Saczewski ,  Shayna Laird ,  Jonne M Laurila ,  Konrad Boblewski ,  Artur Lehmann ,  Jianteng Gu ,  Helena Watts
Affiliations
  • 1. Department of Chemical Technology of Drugs, Medical University of Gdańsk, Al. Gen. J. Hallera 107, Gdańsk 80-416, Poland. [email protected]
PMID: 22172308 DOI: 10.1016/j.bmc.2011.11.025
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.