title: Synthesis and blocking activities of isoindolinone- and isobenzofuranone-containing phenoxylalkylamines as potent α(1)-adrenoceptor antagonists.
abstract: This paper describes the synthesis and blocking activities of twelve new isoindolinone- and isobenzofuranone-containing phenoxylalkylamines as potent α(1)-Adrenoceptor antagonists. These compounds were synthesized in moderate to good yields starting from 3,4-dimethylphenol, and characterized with (1)H-NMR, MS, IR and elemental analysis. Their blocking activities toward α(1)-Adrenoceptors were evaluated on isolated rat anococcygeus muscles. The results indicated that these compounds were very strong in blocking α(1)-Adrenoceptors, and most of them exhibited activities that were comparable to that of known potent α(1)-Adrenoceptor antagonist 1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (DDPH).
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, China.
authors.forename: Shou-Hua
authors.initials: SH
authors.lastname: Zhang
authors.forename: Chun-Ye
authors.initials: CY
authors.lastname: Wang
authors.forename: Zhen-Zhou
authors.initials: ZZ
authors.lastname: Jiang
authors.forename: Pei-Zhou
authors.initials: PZ
authors.lastname: Ni
authors.forename: Jin-Pei
authors.initials: JP
authors.lastname: Zhou
authors.forename: Bao-Min
authors.initials: BM
authors.lastname: Xi
authors.forename: Wen-Hua
authors.initials: WH
authors.lastname: Chen
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000588:Amines / Q000737:chemistry*; D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D054833:Isoindoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D009132:Muscles / Q000378:metabolism; D010627:Phenethylamines / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D000588:Amines; D001572:Benzofurans; D054833:Isoindoles; D010627:Phenethylamines; D011942:Receptors, Adrenergic, alpha; C057485:1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane