5-arylidene-2-imino-4-thiazolidinones : Design and synthesis of novel anti-inflammatory agents
作者： Rosaria Ottanà , Rosanna Maccari , Maria Letizia Barreca , Giuseppe Bruno , Archimede Rotondo
DOI: 10.1016/J.BMC.2005.04.058
关键词:
摘要: The synthesis and pharmacological activity of 5-arylidene-2-imino-4-thiazolidinones (3a-8a) are described. All derivatives exhibited significant levels in models acute inflammation such as carrageenan-induced paw pleurisy edema rats. In particular, 5-(3-methoxyphenylidene)-2-phenylimino-3-propyl-4-thiazolidinone (3a) displayed high inhibition comparable to those indomethacin. addition the ability a new class anti-inflammatory agents inhibit COX isoforms was assessed murine monocyte/macrophage J774 cell line assay. 5-(4-Methoxyphenylidene)-2-phenylimino-3-propyl-4-thiazolidinone (6a), most interesting compound an experiment, docked known active site COX-2 protein showed that its 4-methoxyarylidene moiety can easily occupy secondary pocket considered critical interaction for selectivity.
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