… -activity relationships in prazosin-related compounds. Effect of replacing a piperazine ring with an alkanediamine moiety on. alpha. 1-adrenoreceptor blocking activity

D Giardina, L Brasili, M Gregori, M Massi…

Index: Giardina; Brasili; Gregori; Massi; Picchio; Quaglia; Melchiorre Journal of Medicinal Chemistry, 1989 , vol. 32, # 1 p. 50 - 55

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Citation Number: 23

Abstract

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 ...