2006•PubMedRequires access
[Synthesis and bioactivity of substituted alpha-aminobenzylphosphonate].
Li-zhi Zhao, Ri‐Fang Yang, Rusheng Zhao, Yanfang Zhang, Dong-Mei Chen, Hai Wang
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Abstract
AIM: To search for some substituted alpha-amino phosphonates as leading compounds with the vasodilator effects. METHODS: 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. RESULTS: 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. CONCLUSION: 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.