[取代α-氨基苄基膦酸酯的合成与生物活性]
[Synthesis and bioactivity of substituted alpha-aminobenzylphosphonate].
作者信息
Zhao Li-zhi, Yang Ri-fang, Zhao Ru-sheng, Zhang Yan-fang, Chen Dong-mei, Wang Hai
机构信息
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing, China.
出版信息
Yao Xue Xue Bao. 2006 Apr;41(4):342-5.
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.
目的
寻找一些具有血管舒张作用的取代α-氨基膦酸酯作为先导化合物。
方法
以乙醇为溶剂，通过曼尼希型反应，由苯甲醛、哌嗪和亚磷酸二乙酯制备目标化合物。在离体大鼠主动脉和离体豚鼠回肠中，研究并评估化合物的血管舒张作用以及它们是否激活毒蕈碱受体。
结果
合成了7种取代α-氨基膦酸酯化合物，并通过红外光谱、核磁共振氢谱和元素分析进行了鉴定。其中3种化合物，即化合物2a、2b和2c具有血管舒张活性且不激活M受体。
结论
发现其中两种化合物（2b和2c）具有显著的血管舒张作用，舒张率分别为(67±21)%和(82±18)%。但它们不激活回肠上的M受体。
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