📜2-((5-(Trifluoromethyl)Pyridin-2-yl)Sulfonyl)Ethanaminium Chloride,4-氯苯甲酰氯置于三乙胺体系中,用 二氯甲烷 用作溶剂,以4.25 G的收率获得4-氯-N-[2-[[5-(三氟甲基)-2-吡啶基]磺酰基]乙基]-苯甲酰胺 参考文献:Identification And Characterization Of 4-Chloro-N-(2-{[5-Trifluoromethyl)-2-Pyridyl]Sulfonyl}Ethyl)Benzamide (Gsk3787),A Selective And Irreversible Peroxisome Proliferator-Activated Receptor δ (Pparδ) Antagonist 标题:Identification And Characterization Of 4-Chloro-N-(2-{[5-Trifluoromethyl)-2-Pyridyl]Sulfonyl}Ethyl)Benzamide (Gsk3787),A Selective And Irreversible Peroxisome Proliferator-Activated Receptor δ (Pparδ) Antagonist 摘要:4-Chloro-N-(2-{[5-Trifluoromethyl)-2-Pyridyl]Sulfonyl}Ethyl)Benzamide 3 (Gsk3787) Was Identified As A Potent And Selective Ligand For Ppar Delta Wish Good Pharmacokinetic Properties. A Detailed Binding Study Using Mass Spectral Analysis Confirmed Covalent Binding To Cys249 Within The Ppar Delta Binding Pocket. Gene Expression Studies Showed That Pyridylsulfone 3 Antagonized The Transcriptional Activity Of Ppar Delta And Inhibited Basal Cpt1A Gene Transcription. Compound 3 Is A Ppar Delta Antagonist With Utility As It Tool To Elucidate Ppar Delta Cell Biology And Pharmacology. Doi:10.1021/jm900464J
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合成参考文献
参考文献:10.1016/j.taap.2021.115653 摘要:Venezia O, Islam S, Cho C, Timme-Laragy AR, Sant KE. Modulation of PPAR signaling disrupts pancreas development in the zebrafish, Danio rerio. Toxicology and Applied Pharmacology. 2021 Sep;426():115653. doi: 10.1016/j.taap.2021.115653. 参考文献:10.1021/jm900464j 摘要:Shearer BG, Wiethe RW, Ashe A, Billin AN, Way JM, Stanley TB, Wagner CD, Xu RX, Leesnitzer LM, Merrihew RV, Shearer TW, Jeune MR, Ulrich JC, Willson TM. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. J Med Chem. 2010 Feb 25;53(4):1857–61. doi: 10.1021/jm900464j.