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

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Saczewski J, Hudson A, Scheinin M, Rybczynska A, Ma D, Saczewski F, Laird S, Laurila JM, Boblewski K, Lehmann A, Gu J, Watts H

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. Epub 2011 Nov 25.

PubMed ID

22172308 [ View in PubMed

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Abstract

A series of 2-[(heteroaryl)methyl]imidazolines was synthesized and tested for their activities at alpha(1)- and alpha(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 alpha(1)- and alpha(2)-adrenoceptors. However, their intrinsic activities at alpha(2A)-adrenoceptors proved to be negligible. A selected 7-chloro derivative behaved as a potent alpha(1)-adrenoceptor antagonist and exhibited peripherally mediated hypotensive effects in rats.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clonidine	Alpha-2A adrenergic receptor	EC 50 (nM)	30	N/A	N/A	Details
Norepinephrine	Alpha-2A adrenergic receptor	EC 50 (nM)	118	N/A	N/A	Details