Structure-activity relationships in 1,4-benzodioxan-related compounds. 2. Role of the amine function on alpha-adrenoreceptor blocking activity.

Several WB4101 (1)-related compounds were synthesized. Their alpha-adrenoreceptor blocking properties were evaluated in order to understand the kind of interaction occurring between the amine function of (1)-related compounds and the alpha-adrenoreceptor anionic site. The results suggest that a charge reinforced hydrogen bond rather than an ion pairing might play a most important role in receptor binding.