Synthesis and anti alpha-adrenoceptor activity in vitro of 4-((4-((2-substitutedphenoxy)ethyl)-1-piperazinyl) methyl)- 1,2-dihydro-quinoline-2-one compounds / 药学学报

ABSTRACT

<p><b>AIM</b>To study the synthesis and anti alpha-adrenoceptor activity of 1,2-dihydro-quinoline-2-one compounds.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>Compounds IV3, IV4 and IV6 showed inhibitiion activity, and were worth further studying.</p>