[摘要]：Tamsulosin (-)-1 is the most utilized alpha(1)-adrenoceptor antagonist in the benign prostatic hyperplasia therapy owing to its uroselective antagonism and capability in relieving both obstructive and irritative lower urinary tract symptoms. Here we report the synthesis and pharmacological study of the homochiral (-)-1 analogues (-)-2-(-)-5, bearing definite modifications in the 2-substituted phenoxyethylamino group in order to evaluate their influence on the affinity profile for alpha(1)-adrenoceptor subtypes. The benzyl analogue (-)-3, displaying a preferential antagonist profile for alpha(1A)-than alpha(1D)-and alpha(1B)-adrenoceptors, and a 12-fold higher potency at alpha(1A)-adrenoceptors with respect to the alpha(1B) subtype, may have improved uroselectivity compared to (-)-1. (C) 2010 Elsevier Masson SAS. All rights reserved.
