Synthesis and bioactivity of substituted alpha-aminobenzylphosphonate / 药学学报

ABSTRACT

<p><b>AIM</b>To search for some substituted alpha-amino phosphonates as leading compounds with the vasodilator effects.</p><p><b>METHODS</b>Target compounds were prepared from benzyl aldehyde, piperazine and diethyl phosphite using alcohol as solvent via Mannich-type reaction. In isolated rat aorta and in isolated guinea pig ileum, the vasodilator effects of compounds were investigated and evaluated whether they activated muscarine receptor.</p><p><b>RESULTS</b>Seven compounds of substituted alpha-amino phosphonates have been synthesized and identified by IR, 1H NMR and elemental analysis. Three of them, compound 2a, 2b and 2c have vasodilator activity and do not activate M receptor.</p><p><b>CONCLUSION</b>Two (2b and 2c) of them were found to have the notable vasodilator effect, and the rates of relaxing are (67 +/- 21) % and (82 +/- 18)%, separately. But they did not activate M receptors on ileum.</p>