Synthesis and Blocking Activities of Isoindolinone- and Isobenzofuranone-Containing Phenoxylalkylamines as Potent α1-Adrenoceptor Antagonists

Shou-Hua Zhang; Chun-Ye Wang; Zhen-Zhou Jiang; Pei-Zhou Ni; Jin-Pei Zhou; Bao-Min Xi; Wen-Hua Chen

doi:10.1248/cpb.59.96

Regular Articles

Synthesis and Blocking Activities of Isoindolinone- and Isobenzofuranone-Containing Phenoxylalkylamines as Potent α₁-Adrenoceptor Antagonists

Shou-Hua Zhang, Chun-Ye Wang, Zhen-Zhou Jiang, Pei-Zhou Ni, Jin-Pei Zhou, Bao-Min Xi, Wen-Hua Chen

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Keywords: α₁-Adrenoceptor antagonist, phenoxylalkylamine, synthesis, blocking activity

JOURNAL FREE ACCESS

2011 Volume 59 Issue 1 Pages 96-99

DOI https://doi.org/10.1248/cpb.59.96

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Abstract

This paper describes the synthesis and blocking activities of twelve new isoindolinone- and isobenzofuranone-containing phenoxylalkylamines as potent α₁-Adrenoceptor antagonists. These compounds were synthesized in moderate to good yields starting from 3,4-dimethylphenol, and characterized with ¹H-NMR, MS, IR and elemental analysis. Their blocking activities toward α₁-Adrenoceptors were evaluated on isolated rat anococcygeus muscles. The results indicated that these compounds were very strong in blocking α₁-Adrenoceptors, and most of them exhibited activities that were comparable to that of known potent α₁-Adrenoceptor antagonist 1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (DDPH).

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