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

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概要

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• 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).

著者

• Zhang Shou-Hua

  School of Pharmaceutical Sciences, Southern Medical University

• Wang Chun-Ye

  School of Pharmaceutical Sciences, Southern Medical University

• Jiang Zhen-Zhou

  National Drug Screening Center, China Pharmaceutical University

• Ni Pei-Zhou

  Department of Organic Chemistry, China Pharmaceutical University

• Zhou Jin-Pei

  Center of Drug Discovery, China Pharmaceutical University

• Xi Bao-Min

  School of Pharmaceutical Sciences, Southern Medical University

• Chen Wen-Hua

  School of Pharmaceutical Sciences, Southern Medical University

関連論文

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