Synthesis and bioactivity of substituted α-aminobenzylphosphonate

AimTo search for some substituted α-amino phosphonates as leading compounds with the vasodilator effects. MethodsTarget 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. ResultsSeven compounds of substituted α-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. ConclusionTwo (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.