[Synthesis and vasodilative activities of alpha-phenylcinnamide].
OBJECTIVE
To search for compounds having strong vasodilating effect.


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.


CONCLUSIONS
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.
Mou
L Y
LY
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
Lin
Z Y
ZY
Zhu
L Y
LY
Liang
X T
XT
D000818:Animals; D002934:Cinnamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051668:Delayed Rectifier Potassium Channels; D015394:Molecular Structure; D015221:Potassium Channels / Q000378:metabolism; D024642:Potassium Channels, Voltage-Gated; D051381:Rats; D014661:Vasoconstriction / Q000187:drug effects*; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D002934:Cinnamates; D051668:Delayed Rectifier Potassium Channels; D015221:Potassium Channels; D024642:Potassium Channels, Voltage-Gated; D014665:Vasodilator Agents