Synthesis and anti-inflammatory activity of hydroxylated E,E-1-(3'-indolyl)-5-(substituted phenyl)-1,4-pentadien-3-one derivatives.
- Author:
Xiao-he GUO
1
;
Sen-xiang CHENG
;
Gui-fang CHENG
;
Jing-xi XIE
;
Jun-biao CHANG
Author Information
- Publication Type:Journal Article
- MeSH: Alkadienes; chemical synthesis; pharmacology; Animals; Anti-Inflammatory Agents; chemical synthesis; pharmacology; Indoles; chemical synthesis; pharmacology; Macrophages, Peritoneal; cytology; metabolism; Male; Mice; Tumor Necrosis Factor-alpha; secretion
- From: Acta Pharmaceutica Sinica 2006;41(4):346-351
- CountryChina
- Language:Chinese
-
Abstract:
AIMA 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.
METHODSE,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.
RESULTSPreliminary in vitro pharmacological tests showed that all compounds exhibited anti-inflammatory activity.
CONCLUSIONCompounds 4d and 4e exhibited potent anti-inflammatory activity and their anti-inflammatory activity was comparable to resveratrol, and were worthy of further study.
