e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
… -activity relationships in prazosin-related compounds. Effect of replacing a piperazine ring with an alkanediamine moiety on. alpha. 1-adrenoreceptor blocking activity
Several prazosin-related compounds were synthesized in which the piperazine ring of prazosin (1) was replaced by an alkanediamine chain and were evaluated for their blocking activity on al-and a2-adrenoreceptors in isolated rat vas deferens. All the compounds investigated proved highly selective toward the al-adrenoreceptor owing to a very low affinity for a2-adrenoreceptors. Furthermore, compounds 2, 9, and 13 were also investigated in ...