Synthesis and Biological Activities of Novel 1,2,3,5-Tetrahydroimidazo2,1-bquinazoline Derivatives

摘要

A series of variously substituted 1,2,3,5-tetrahydroimidazo2,1-bquinazoline derivatives 3-4 and 6-7 were prepared by the reactions of 2-chloro-4,5-dihydroimidazole (1) with the appropriate 2-aminophenyl ketones 2 and 5.The structures of the new compounds obtained were determined by elemental analysis as well as IR and NMR spectroscopic data.Biological activities of the compounds 3 and 6 was examined on P_2 membrane preparations obtained from rat whole brains and rat tail artery.Among the compounds tested,5-methylidene-l,2,3,5-tetrahydroimidazo2,l-bquinazoline (6a) showed high and moderate binding affinities to I_2 imidazoline (KAPPA_i=5.2 nM) and alpha_2-adrenergic (KAPPA_i=149 nM) receptors,respectively.