Evaluation of caffeic acid amide analogues as anti-platelet aggregation and anti-oxidative agents.
A series of amides of caffeic acid were synthesized and evaluated for their anti-platelet and anti-oxidative activities. N-(2-Bromo-phenyl)-3-(3,4-dihydroxy-phenyl)-acrylamide (12) and N-(3-Bromo-phenyl)-3-(3,4-dihydroxy-phenyl)-acrylamide (13) exhibited potent inhibitory activity (IC(50)=5.8 and 6.7 microM, respectively) against arachidonic acid-induced (AA) platelet aggregation, comparable with invalid caffeic acid. Most of the synthesized caffeic acid anilides exhibited the promising anti-platelet aggregation in AA-induced assay and anti-oxidative activities. This study also exhibited that caffeic anilides displayed more potent anti-oxidative activity in the radical scavenging activity assay than trolox and vitamin E.
Hung
Chia-Cheng
CC
National Research Institute of Chinese Medicine, Shin-Pai, Taipei 112, Taiwan.
Tsai
Wei-Jen
WJ
Kuo
Li-Ming Yang
LM
Kuo
Yao-Haur
YH
D000577:Amides / Q000737:chemistry; D000818:Animals; D000975:Antioxidants / Q000494:pharmacology*; D001792:Blood Platelets / Q000187:drug effects; D002109:Caffeic Acids / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011817:Rabbits; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared
D000577:Amides; D000975:Antioxidants; D002109:Caffeic Acids; D010975:Platelet Aggregation Inhibitors; C040048:caffeic acid