A1 Refereed original research article in a scientific journal
Synthesis and pharmacological properties of 4(5)-(2-ethyl-2,3-dihydro-2-silainden-2-yl)imidazole, a silicon analogue of atipamezole
Authors: Heinonen P, Sipila H, Neuvonen K, Lonnberg H, Cockcroft VB, Wurster S, Virtanen R, Savola MKT, Salonen JS, Savola JM
Publisher: EDITIONS SCIENTIFIQUES ELSEVIER
Publication year: 1996
Journal:: European Journal of Medicinal Chemistry
Journal name in source: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Journal acronym: EUR J MED CHEM
Volume: 31
Issue: 9
First page : 725
Last page: 729
Number of pages: 5
ISSN: 0223-5234
DOI: https://doi.org/10.1016/0223-5234(96)85882-X
Abstract
4(5)-(2-Ethyl-2,3-dihydro-2-silainden-2-yl)imidazole 2a, 4(5)-(2-methyl-2,3-dihydro-2-silainden-2-yl)imidazole 2b and 4(5)-(2-ethyl-2,3-dihydro-2-silainden-2-yl)-2-methylimidazole 2c, C2 silicon analogues of the commercially available alpha(2)-adrenergic receptor antagonist atipamezole 1, were prepared and their pharmacological properties were evaluated. The results show that 2a retained significant affinity for the receptors, and the in vivo pharmacokinetic properties of 2a were comparable to those of 1.
4(5)-(2-Ethyl-2,3-dihydro-2-silainden-2-yl)imidazole 2a, 4(5)-(2-methyl-2,3-dihydro-2-silainden-2-yl)imidazole 2b and 4(5)-(2-ethyl-2,3-dihydro-2-silainden-2-yl)-2-methylimidazole 2c, C2 silicon analogues of the commercially available alpha(2)-adrenergic receptor antagonist atipamezole 1, were prepared and their pharmacological properties were evaluated. The results show that 2a retained significant affinity for the receptors, and the in vivo pharmacokinetic properties of 2a were comparable to those of 1.
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