CAS: 317318-84-6; 2-(4-(((2-(3-Fluoro-4-(Trifluoromethyl)Phenyl)-4-Methylthiazol-5-yl)Methyl)Thio)-2-Methylphenoxy)Acetic Acid

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CAS号876-02-8 4-羟基-3-甲基苯乙酮 | CAS号56077-47-5 methyl 2-(2-met... | CAS号317319-10-1 2-(4-羟基-2-甲基苯氧基)乙酸甲酯 | CAS号166953-80-6 Acetic acid, 2-... | CAS号317319-09-8 (4-acetoxy-2-me... | CAS号583883-84-5 methyl 2-(4-((d... | CAS号317319-33-8 5-(CHLOROMETHYL... | CAS号317319-27-0 (2-(3-FLUORO-4-... | CAS号317319-21-4 2-[3-氟-(三氟甲基)苯基...

2-溴-4-甲基-1,3-噻唑-5-甲酸乙酯置于sodium Tetrahydroborate,氯化亚砜,Sodium Carbonate,Caesium Carbonate,三氟乙酸体系中,用 乙二醇二甲醚,乙醇,二氯甲烷,氯仿,水,乙腈 用作溶剂,化学反应 34.5H,反应生成2-(4-(((2-(3-氟-4-(三氟甲基)苯基)-4-甲基噻唑-5-基)甲基)硫代)-2-甲基苯氧基)乙酸
参考文献:Parallel Chemistry Approach To Identify Novel Nuclear Receptor Ligands Based On The Gw0742 Scaffold
标题:Parallel Chemistry Approach To Identify Novel Nuclear Receptor Ligands Based On The Gw0742 Scaffold
摘要:We Describe The Parallel Synthesis Of Novel Analogs Of Gw0742,A Peroxisome Proliferator-Activated Receptor Delta (Ppar Delta) Agonist For That Purpose,Modified Reaction Conditions Were Applied,Such As A Solid-Phase Palladium-Catalyzed Suzuki Coupling. In Addition,Tetrazole-Based Compounds Were Generated As A Bioisostere For Carboxylic Acid-Containing Ligand Gw0742. The New Compounds Were Investigated For Their Ability To Activate Ppar Delta Mediated Transcription And Their Cross-Reactivity With The Vitamin D Receptor (Vdr),Another Member Of The Nuclear Receptor Superfamily. We Identified Many Potent Ppar Delta Agonists That Were Less Toxic Than Gw0742,Where Similar To 65 Of The Compounds Synthesized Exhibited Partial Ppar Delta Activity (23-98%) With Ec50 Values Ranging From 0.007-18.2 Mu M. Some Ligands,Such As Compound 32,Were More Potent Inhibitors Of Vdr-Mediated Transcription With Significantly Reduced Ppar Delta Activity Than Gw0742,However,None Of The Ligands Were Completely Selective For Vdr Inhibition Over Ppar Delta Activation Of Transcription.
Doi:10.1021/acscombsci.7B00066