📜2-氯乙酰乙酸乙酯,3-氟-4-(三氟甲基)硫代苯甲酰胺 以 乙醇 作为反应溶剂,以65%的收率获得产物乙基2-[3-氟-(三氟甲基)苯基]-4-甲基-噻唑-5-羧酸酯
参考文献:Novel Selective Small Molecule Agonists For Peroxisome Proliferator-Activated Receptor δ (Pparδ)-synthesis And Biological Activity
标题:Novel Selective Small Molecule Agonists For Peroxisome Proliferator-Activated Receptor δ (Pparδ)-synthesis And Biological Activity
摘要:We Report The Synthesis And Biological Activity Of A New Series Of Small Molecule Agonists Of The Human Peroxisome Proliferator-Activated Receptor Delta (Ppardelta). Several Hits Were Identified From Our Original Libraries Containing Lipophilic Carboxylic Acids. Optimization Of These Hits By Structure-Guided Design Led To 7K (Gw501516) And 71 (Gw0742),Which Shows An Ec50 Of 1.1 Nm Against Ppardelta With 1000-Fold Selectivity Over The Other Human Subtypes. (C) 2003 Elsevier Science Ltd. All Rights Reserved.
DOI:10.1016/s0960-894X(03)00207-5