Structure–Activity relationships among novel phenoxybenzamine-Related β-Chloroethylamines

D Giardina, M Crucianelli, P Angeli, M Buccioni…

文献索引：Giardina, Dario; Crucianelli, Mauro; Angeli, Piero; Buccioni, Michela; Gulini, Ugo; Marucci, Gabriella; Sagratini, Gianni; Melchiorre, Carlo Bioorganic and medicinal chemistry, 2002 , vol. 10, # 5 p. 1291 - 1303

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被引用次数: 6

摘要

A series of β-chloroethylamines 5–18, structurally related to the irreversible α1-adrenoceptor antagonist phenoxybenzamine [PB, N-benzyl-N-(2-chloroethyl)-N-(1-methyl-2- phenoxyethyl) amine hydrochloride, 1] and the competitive antagonist WB4101 [N-(2, 3- dihydro-1, 4-benzodioxin-2-ylmethyl)-N-[2-(2, 6-dimethoxyphenoxy) ethyl] amine hydrochloride, 2], were synthesized and evaluated for their activity at α-adrenoceptors of ...