[Synthesis and anti alpha-adrenoceptor activity in vitro of 4-((4-((2-substitutedphenoxy)ethyl)-1-piperazinyl) methyl)- 1,2-dihydro-quinoline-2-one compounds].
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.
Liu
Hui
H
Department of Medical Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Ran
Chong-zhao
CZ
Xia
Lin
L
Ni
Pei-zhou
PZ
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
D000317:Adrenergic alpha-Antagonists; D010627:Phenethylamines; D015363:Quinolones; D011942:Receptors, Adrenergic, alpha; C057485:1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane