New imidazoline/α(2)-adrenoceptors affecting compounds-4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. Synthesis and receptor affinity studies

Bioorg Med Chem. 2011 Jan 1;19(1):156-67. doi: 10.1016/j.bmc.2010.11.039. Epub 2010 Nov 25.

Abstract

Compilation of agmatine structure and imidazoline moiety leads to a new group of imidazoline/α(2)-adrenoceptor ligands, 4(5)-(2-aminoethyl)imidazoline derivatives. In this study the exploration of previously unknown 4(5)-(2-aminoethyl)imidazolines including the analogues of reported imidazoline and α(2)-aderenoceptors ligands: clonidine, rilmenidine, idazoxan, efaroxan, antazoline, tracizoline is described. The synthesis of a variety of novel 4(5)-(2-aminoethyl)imidazolines and their I(1), I(2), α(2)-adrenoceptors affinities are reported.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Imidazoles / chemical synthesis
  • Imidazoles / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Receptors, Adrenergic, alpha-2 / drug effects*

Substances

  • Imidazoles
  • Receptors, Adrenergic, alpha-2