SYNTHESIS AND VASODILATIVE ACTIVITIES OF CINNAMIDE AND α-PHENYLCINNAMIDE DERIVATIVES

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.