Structural exploration, synthesis and pharmacological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives as iNOS inhibitors against inflammatory diseases

In our previous work, 3I inhibited the LPS-induced iNOS activity and NO production in RAW 264.7 cells and improved joint inflammation and cartilage destruction in inflammatory model. In this study, we synthesized 59 derivatives and bioisosteres on the basis of 3I by Knoevenagel condensation and biol...

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Veröffentlicht in:	European journal of medicinal chemistry 2015-03, Vol.92, p.178-190
Hauptverfasser:	Ma, Liang, Pei, Heying, Lei, Lei, He, Linhong, Chen, Jinying, Liang, Xiaolin, Peng, Aihua, Ye, Haoyu, Xiang, Mingli, Chen, Lijuan
Format:	Artikel
Sprache:	eng
Schlagworte:	5-Benzylidenethiazolidine-2,4-dione Animals Benzylidene Compounds - chemical synthesis Benzylidene Compounds - chemistry Benzylidene Compounds - pharmacology Carrageenan Cell Line Dose-Response Relationship, Drug Edema - chemically induced Edema - drug therapy Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Female Inducible nitric oxide synthase Inflammation Inflammation - drug therapy Lipopolysaccharides - antagonists & inhibitors Lipopolysaccharides - pharmacology Male Mice Mice, Inbred ICR Molecular Structure Nitric oxide Nitric Oxide - antagonists & inhibitors Nitric Oxide - biosynthesis Nitric Oxide Synthase Type II - antagonists & inhibitors Nitric Oxide Synthase Type II - metabolism Paw edema Rats Rats, Inbred Lew Structure-Activity Relationship Thiazolidinediones - chemical synthesis Thiazolidinediones - chemistry Thiazolidinediones - pharmacology
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