Design, synthesis and molecular modeling of novel D-ring substituted steroidal 4,5-dihydropyrazole thiazolinone derivatives as anti-inflammatory agents by inhibition of COX-2/iNOS production and down-regulation of NF-κB/MAPKs in LPS-induced RAW264.7 macrophage cells

It has been reported that 4,5-dihydropyrazole and thiazole derivatives have many biological functions, especially in the aspect of anti-inflammation. According to the strategy of pharmacophore combination, we introduced thiazolinone and dihydropyrazole moiety into steroid skeleton to design and synt...

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Veröffentlicht in:	European journal of medicinal chemistry 2024-06, Vol.272, p.116460-116460, Article 116460
Hauptverfasser:	Cai, Xiaorui, Cai, Jianfeng, Fang, Ling, Xu, Siqi, Zhu, Huide, Wu, Shuteng, Chen, Yicun, Fang, Shuopo
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-inflammatory Anti-Inflammatory Agents - chemical synthesis Anti-Inflammatory Agents - chemistry Anti-Inflammatory Agents - pharmacology Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology Cyclooxygenase 2 - metabolism Cyclooxygenase 2 Inhibitors - chemical synthesis Cyclooxygenase 2 Inhibitors - chemistry Cyclooxygenase 2 Inhibitors - pharmacology Cytotoxicity Dihydropyrazole Dose-Response Relationship, Drug Down-Regulation - drug effects Drug Design Lipopolysaccharides - antagonists & inhibitors Lipopolysaccharides - pharmacology Macrophages - drug effects Macrophages - metabolism Mice Mitogen-Activated Protein Kinases - antagonists & inhibitors Mitogen-Activated Protein Kinases - metabolism Models, Molecular Molecular Docking Simulation Molecular Structure NF-kappa B - antagonists & inhibitors NF-kappa B - metabolism Nitric Oxide Synthase Type II - antagonists & inhibitors Nitric Oxide Synthase Type II - metabolism Pregnenolone Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology RAW 264.7 Cells RAW 264.7 cells Steroid Steroids - chemical synthesis Steroids - chemistry Steroids - pharmacology Structure-Activity Relationship Thiazoles - chemical synthesis Thiazoles - chemistry Thiazoles - pharmacology Thiazolinone
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