Synthesis and anti alpha-adrenoceptor activity in vitro of 4-((4-((2-substitutedphenoxy)ethyl)-1-piperazinyl) methyl)- 1,2-dihydro-quinoline-2-one compounds.
- Author:
Hui LIU
1
;
Chong-zhao RAN
;
Lin XIA
;
Pei-zhou NI
Author Information
- Publication Type:Journal Article
- MeSH: Adrenergic alpha-Antagonists; chemical synthesis; pharmacology; Animals; Aorta; drug effects; In Vitro Techniques; Molecular Structure; Phenethylamines; chemical synthesis; pharmacology; Quinolones; chemical synthesis; pharmacology; Rabbits; Receptors, Adrenergic, alpha; drug effects; metabolism; Technology, Pharmaceutical
- From: Acta Pharmaceutica Sinica 2002;37(3):181-185
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo study the synthesis and anti alpha-adrenoceptor activity of 1,2-dihydro-quinoline-2-one compounds.
METHODSAcylation, 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.
RESULTSTwelve 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.
CONCLUSIONCompounds IV3, IV4 and IV6 showed inhibitiion activity, and were worth further studying.
