Relationship between chemical structure, binding affinity and selectivity towards [alpha]1-adrenoceptors in the group of substituted n-phenylpiperazines. Part 2. compounds containing ethane-1,2-diyl connecting chain

Relationship between chemical structure, binding affinity and selectivity towards α[1]-adrenoceptors in the group of substituted [n]-phenylpiperazines. Part 2[*]. compounds containing ethane-1,2-diyl connecting chain The [N]-phenylpiperazine structures exhibit very extensive multiple receptor activities including the influencing of α[1]-adrenoceptors (α[1]-AR). Their antagonistic activity towards α[1]-AR is intensively applied in the therapy of cardiovascular system diseases - e. g. hypertension as well as in the treatment of benign prostatic hyperplasia. The limited ratio of selective effect on the specific subtypes of the α[1]-AR by certain drugs used in the practice (azosine-type structures) leads to multiple side effects which includes postural hypotension, syncope or first dose phenomena. The existence of multiple α[1]-AR subtypes holds promise for the discovery, projection and development of more specific selective drug molecules targeting only one α[1]-adrenoceptor subtype and making them free from side effects. Towards this aim wide-ranging modifications have been reported in the literature on the "basic" structure of the [N]-phenylpiperazine-based molecules. The present paper deals with the affinity features of (substituted) [N]-phenylpiperazines towards α[1]-ARs in which the structure is a connecting chain formed by (unsubstituted) ethane-1,2-diyl moiety bonded through certain atom or group (S, O, NH, NHCO-fragment, respectively) at the lipophilic part of the molecule. [PUBLICATION ABSTRACT]