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Synthesis and pharmacological properties of 4(5)-(2-ethyl-2,3-dihydro-2 silainden-2-yl)imidazole, a silicon analogue of atipamezole

Authors :
Siegfried Wurster
K. Neuvonen
M. K. T. Savola
Harri Lönnberg
Juha-Matti Savola
Victor Cockcroft
Petri Heinonen
J. S. Salonen
H. Sipilä
Raimo Virtanen
Source :
European Journal of Medicinal Chemistry. 31:725-729
Publication Year :
1996
Publisher :
Elsevier BV, 1996.

Abstract

Summary 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 α 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 .

Details

ISSN :
02235234
Volume :
31
Database :
OpenAIRE
Journal :
European Journal of Medicinal Chemistry
Accession number :
edsair.doi...........c3934d7bf83ff33f550730f1f9c3030b
Full Text :
https://doi.org/10.1016/0223-5234(96)85882-x