Structure-activity relationships in prazosin-related compounds. 2. Role of the piperazine ring on. alpha.-blocking activity

…, U Gulini, M Massi, MG Piloni, P Pompei…

Index: Giardina, Dario; Gulini, Ugo; Massi, Maurizio; Piloni, Maria G.; Pompei, Pierluigi; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 6 p. 690 - 698

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Citation Number: 52

Abstract

Several prazosin-related compounds have been synthesized and evaluated for their blocking activity toward a-adrenoreceptors. The structural modification performed on the prazosin structure included the replacement of the piperazine ring with 2, 3- dialkylpiperazine or 1, 2-~ yclohexanediamine moieties to characterize a lipophilic binding pocket in the al-adrenoreceptor surface. Cyclohexanediamine derivatives 3-6 were almost ...