Aim: To search for compounds having strong vasodilating effect.
Methods and results: The mixed anhydride and alpha-phenylcinnamyl halide were used. Twenty-two alpha-phenylcinnamide derivatives were synthesized. The strutures were elucidated on the basis of MS and 1HNMR. Compounds 1-22 are new compounds.
Conclusion: Vasodilative activity assays were conducted for the target compounds and the results indicated that several compounds (3, 9 and 11) demonstrated superior pharmacological profiles to the lead compound, among which compound 11 was further evaluated and found to be indicative of potential KCO activity. Preliminary SAR of alpha-phenylcinnamides was discussed herein.