4-Substitutedphthalazines and phthalazinones: synthesis, characterization and beta-adrenergic blocking activity

Abstract

Novel 4-(4-bromophenyl)phthalazine and phthalazinone derivatives connected through 2-propanol spacer to N-substituted piperazine residue were synthesized. All the new compounds were screened for their effect on β-adrenergic blocking activity on the norepinephrine-induced precontracted aortic ring module. Most test compounds displayed appreciable β-adrenolytic activity compared to propranolol as a reference standard. The results have shown that compounds 3a, 3d, 3e and 7c displayed appreciable inhibition of norepinephrine-induced aortic ring contraction. Graphical Abstract: A novel 4-(4-bromophenyl)phthalazine and phthalazinone derivatives connected through 2-propanol spacer to N-substituted piperazine residue were synthesized. All new compounds were screened for their effect on β-adrenergic blocking activity on the norepinephrine-induced precontracted aortic ring module.[Figure not available: see fulltext.] © 2012 Springer Science+Business Media, LLC.