[Synthesis and anti-inflammatory activity of hydroxylated E,E-1-(3'-indolyl)-5-(substituted phenyl)-1,4-pentadien-3-one derivatives].
OBJECTIVE
A series of new 1,4-pentadien-3-one derivatives were synthesized to search for new Eight novel hydroxylated non-steroidal anti-inflammatory drugs (NSAIDs) with potent activity.


METHODS
E,E-1-(3'-indolyl)-5-( substituted phenyl)-1,4-pentadien-3-one derivatives were synthesized by means of aldol condensation and characterized by 1H NMR, ESI-MS and element analysis. Their anti-inflammatory activity in vitro were evaluated.


RESULTS
Preliminary in vitro pharmacological tests showed that all compounds exhibited anti-inflammatory activity.


CONCLUSIONS
Compounds 4d and 4e exhibited potent anti-inflammatory activity and their anti-inflammatory activity was comparable to resveratrol, and were worthy of further study.
Guo
Xiao-he
XH
Department of Chemistry , University of Science and Technology of China, Hefei.
Cheng
Sen-xiang
SX
Cheng
Gui-fang
GF
Xie
Jing-xi
JX
Chang
Jun-biao
JB
D000466:Alkadienes / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D017737:Macrophages, Peritoneal / Q000166:cytology / Q000378:metabolism*; D008297:Male; D051379:Mice; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism*
D000466:Alkadienes; D000893:Anti-Inflammatory Agents; D007211:Indoles; D014409:Tumor Necrosis Factor-alpha