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Updated: May 26, 2026

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Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines
Jaroslaw Saczewski1, Alan Hudson, Mika Scheinin
1Department of Chemical Technology of Drugs, Medical University of Gdańsk, Al. Gen. J. Hallera 107, Gdańsk 80-416, Poland. js@gumed.edu.pl
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.
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