Abstract
Relationship between biological responses and binding affinities at I1/I2/I3 imidazoline receptors of compounds with imidazoline, pyrroline or oxazoline moieties was studied by 2D-QSAR, 3D-QSAR and quantitative pharmacophore development approaches. Since the I1 imidazoline receptor is involved in central inhibition of sympathicus that produce hypotensive effect, the I2 receptor is allosteric modulator of monoamine oxidase B (MAO-B) and the I3 receptor regulates insulin secretion from pancreatic β-cells, design and synthesis of selective I1/I2/I3 imidazoline ligands are very important for the development of new effective therapeutic agents. New agonists and antagonists with high selectivity for I1/I2/I3 imidazoline receptor classes have been recently synthesized and examined. The present review will highlight the main chemical diversity and pharmacophore features of selective I1/I2/I3 imidazoline receptor ligands.
Keywords: I1-imidazoline receptors, I2-imidazoline receptors, I3-imidazoline receptors, hypotensive, enzymes, phenylethanolamine-Nmethyl, imidazoline, imidazole-4-acetic, agmatine, lipophilicity
Mini-Reviews in Medicinal Chemistry
Title:Pharmacophore Development and SAR Studies of Imidazoline Receptor Ligands
Volume: 12 Issue: 14
Author(s): Katarina Nikolic and Danica Agbaba
Affiliation:
Keywords: I1-imidazoline receptors, I2-imidazoline receptors, I3-imidazoline receptors, hypotensive, enzymes, phenylethanolamine-Nmethyl, imidazoline, imidazole-4-acetic, agmatine, lipophilicity
Abstract: Relationship between biological responses and binding affinities at I1/I2/I3 imidazoline receptors of compounds with imidazoline, pyrroline or oxazoline moieties was studied by 2D-QSAR, 3D-QSAR and quantitative pharmacophore development approaches. Since the I1 imidazoline receptor is involved in central inhibition of sympathicus that produce hypotensive effect, the I2 receptor is allosteric modulator of monoamine oxidase B (MAO-B) and the I3 receptor regulates insulin secretion from pancreatic β-cells, design and synthesis of selective I1/I2/I3 imidazoline ligands are very important for the development of new effective therapeutic agents. New agonists and antagonists with high selectivity for I1/I2/I3 imidazoline receptor classes have been recently synthesized and examined. The present review will highlight the main chemical diversity and pharmacophore features of selective I1/I2/I3 imidazoline receptor ligands.
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Cite this article as:
Nikolic Katarina and Agbaba Danica, Pharmacophore Development and SAR Studies of Imidazoline Receptor Ligands, Mini-Reviews in Medicinal Chemistry 2012; 12 (14) . https://dx.doi.org/10.2174/138955712803832636
DOI https://dx.doi.org/10.2174/138955712803832636 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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