title: [Synthesis and anti alpha-adrenoceptor activity in vitro of 4-((4-((2-substitutedphenoxy)ethyl)-1-piperazinyl) methyl)- 1,2-dihydro-quinoline-2-one compounds].
abstract: OBJECTIVE
  To study the synthesis and anti alpha-adrenoceptor activity of 1,2-dihydro-quinoline-2-one compounds.
  
  
  METHODS
  Acylation, bromination and cyclization, and substitute reactions were used in the synthesis of the title compounds IV. A proposed mechanism was showed to explain the unusual compounds 5 and 6 in the route C. The inhibition activity of the six target compounds were tested.
  
  
  RESULTS
  Twelve new compounds were synthesized (II1-6 and IV1-6). Among them, six new compounds (IV1-6) are the title compounds. Structure of the title compounds were determined by IR, 1HNMR, MS and HRMS.
  
  
  CONCLUSIONS
  Compounds IV3, IV4 and IV6 showed inhibitiion activity, and were worth further studying.
authors.affiliation: Department of Medical Chemistry, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Liu
authors.forename: Chong-zhao
authors.initials: CZ
authors.lastname: Ran
authors.forename: Lin
authors.initials: L
authors.lastname: Xia
authors.forename: Pei-zhou
authors.initials: PZ
authors.lastname: Ni
mesh_terms: D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001011:Aorta / Q000187:drug effects; D066298:In Vitro Techniques; D015394:Molecular Structure; D010627:Phenethylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D011817:Rabbits; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism; D013678:Technology, Pharmaceutical
chemical_list: D000317:Adrenergic alpha-Antagonists; D010627:Phenethylamines; D015363:Quinolones; D011942:Receptors, Adrenergic, alpha; C057485:1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane