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

: Heinonen P, Sipila H, Neuvonen K, Lonnberg H, Cockcroft VB, Wurster S, Virtanen R, Savola MKT, Salonen JS, Savola JM

Publisher: EDITIONS SCIENTIFIQUES ELSEVIER

: 1996

: European Journal of Medicinal Chemistry

: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

: EUR J MED CHEM

: 31

: 9

: 725

: 729

: 5

: 0223-5234

DOI: https://doi.org/10.1016/0223-5234(96)85882-X

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.

Chemical sciences