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[Synthesis and vasodilative activities of alpha-phenylcinnamide]
1Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
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.