Pharmacophore Development and SAR Studies of Imidazoline Receptor Ligands
Abstract
Relationship between biological responses and binding affinities at I-1/I-2/I-3 imidazoline receptors of compounds with imidazoline, pyrroline or oxazoline moieties was studied by 2D-QSAR, 3D-QSAR and quantitative pharmacophore development approaches. Since the I-1 imidazoline receptor is involved in central inhibition of sympathicus that produce hypotensive effect, the I-2 receptor is allosteric modulator of monoamine oxidase B (MAO-B) and the I-3 receptor regulates insulin secretion from pancreatic beta-cells, design and synthesis of selective I-1/I-2/I-3 imidazoline ligands are very important for the development of new effective therapeutic agents. New agonists and antagonists with high selectivity for I-1/I-2/I-3 imidazoline receptor classes have been recently synthesized and examined. The present review will highlight the main chemical diversity and pharmacophore features of selective I-1/I-2/I-3 imidazoline receptor ligands.
Keywords:
I1-imidazoline receptors / I2-imidazoline receptors / I3-imidazoline receptorsSource:
Mini-Reviews in Medicinal Chemistry, 2012, 12, 14, 1542-1555Publisher:
- Bentham Science Publ Ltd, Sharjah
Funding / projects:
DOI: 10.2174/138955712803832636
ISSN: 1389-5575
PubMed: 22512575
WoS: 000311955300010
Scopus: 2-s2.0-84873156974
Collections
Institution/Community
PharmacyTY - JOUR AU - Nikolić, Katarina AU - Agbaba, Danica PY - 2012 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1691 AB - Relationship between biological responses and binding affinities at I-1/I-2/I-3 imidazoline receptors of compounds with imidazoline, pyrroline or oxazoline moieties was studied by 2D-QSAR, 3D-QSAR and quantitative pharmacophore development approaches. Since the I-1 imidazoline receptor is involved in central inhibition of sympathicus that produce hypotensive effect, the I-2 receptor is allosteric modulator of monoamine oxidase B (MAO-B) and the I-3 receptor regulates insulin secretion from pancreatic beta-cells, design and synthesis of selective I-1/I-2/I-3 imidazoline ligands are very important for the development of new effective therapeutic agents. New agonists and antagonists with high selectivity for I-1/I-2/I-3 imidazoline receptor classes have been recently synthesized and examined. The present review will highlight the main chemical diversity and pharmacophore features of selective I-1/I-2/I-3 imidazoline receptor ligands. PB - Bentham Science Publ Ltd, Sharjah T2 - Mini-Reviews in Medicinal Chemistry T1 - Pharmacophore Development and SAR Studies of Imidazoline Receptor Ligands VL - 12 IS - 14 SP - 1542 EP - 1555 DO - 10.2174/138955712803832636 ER -
@article{ author = "Nikolić, Katarina and Agbaba, Danica", year = "2012", abstract = "Relationship between biological responses and binding affinities at I-1/I-2/I-3 imidazoline receptors of compounds with imidazoline, pyrroline or oxazoline moieties was studied by 2D-QSAR, 3D-QSAR and quantitative pharmacophore development approaches. Since the I-1 imidazoline receptor is involved in central inhibition of sympathicus that produce hypotensive effect, the I-2 receptor is allosteric modulator of monoamine oxidase B (MAO-B) and the I-3 receptor regulates insulin secretion from pancreatic beta-cells, design and synthesis of selective I-1/I-2/I-3 imidazoline ligands are very important for the development of new effective therapeutic agents. New agonists and antagonists with high selectivity for I-1/I-2/I-3 imidazoline receptor classes have been recently synthesized and examined. The present review will highlight the main chemical diversity and pharmacophore features of selective I-1/I-2/I-3 imidazoline receptor ligands.", publisher = "Bentham Science Publ Ltd, Sharjah", journal = "Mini-Reviews in Medicinal Chemistry", title = "Pharmacophore Development and SAR Studies of Imidazoline Receptor Ligands", volume = "12", number = "14", pages = "1542-1555", doi = "10.2174/138955712803832636" }
Nikolić, K.,& Agbaba, D.. (2012). Pharmacophore Development and SAR Studies of Imidazoline Receptor Ligands. in Mini-Reviews in Medicinal Chemistry Bentham Science Publ Ltd, Sharjah., 12(14), 1542-1555. https://doi.org/10.2174/138955712803832636
Nikolić K, Agbaba D. Pharmacophore Development and SAR Studies of Imidazoline Receptor Ligands. in Mini-Reviews in Medicinal Chemistry. 2012;12(14):1542-1555. doi:10.2174/138955712803832636 .
Nikolić, Katarina, Agbaba, Danica, "Pharmacophore Development and SAR Studies of Imidazoline Receptor Ligands" in Mini-Reviews in Medicinal Chemistry, 12, no. 14 (2012):1542-1555, https://doi.org/10.2174/138955712803832636 . .