肉桂酰胺及α-苯基肉桂酰胺衍生物的合成及扩血管活性  

SYNTHESIS AND VASODILATIVE ACTIVITIES OF CINNAMIDE AND α PHENYLCINNAMIDE DERIVATIVES

作　　者：何欣[1] 林紫云[1] 朱莉亚[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所

出　　处：《药学学报》1999年第3期192-196,共5页Acta Pharmaceutica Sinica

摘　　要：目的：寻找新型的抗高血压药物。方法：用典型的Ｋｎｏｅｖｅｎａｇｅｌ缩合反应和混合酸酐法合成。结果：合成了９个肉桂酰胺类化合的和８个α取代苯基肉桂酰胺类衍生物，均为新化合物。结论：体外扩血管活性试验表明，在分子的苯环与羰基间引入双键不利于化合物对去甲肾上腺素［以下简称ＮＥ］（１０－７ｍｏｌ·Ｌ－１）引起的大鼠主动脉条收缩抑制活性；AIM: To search for compounds having strong vasodilating effect. METHODS: The classic Knoevenagel condensation and mixed anhydride method were used. RESULTS: Nine cinnamides and eight α phenylcinnamide derivatives were synthesized. CONCLUSION: Vasodilative activity screening in vitro showed that the olefinic linkage inserted between the benzene ring and carbonyl group was unfavourable to the inhibiting activity on noradrenaline (10 -7 mol·L -1 ) induced contraction of rat aortic strip, while the introduction of bulky groups (substituted phenyl) at α position of the cinnamoyl carbonyl group might selectively enhance the inhibiting activity against 85 7 mmol·L -1 KCl induced contraction of rat aortic strip.

关 键 词：肉桂酰胺 α苯基肉桂酰胺 扩血管活性 

分 类 号：R914.5[医药卫生—药物化学] R972.4[医药卫生—药学]