CAS: 223127-49-9; 4-(5-Nitropyridin-2-yl)Benzoic Acid

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864075-95-6 89076-64-2 223127-51-3

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CAS号223127-51-3 methyl 4-(5-nit... | CAS号586-76-5 对溴苯甲酸 | CAS号619-42-1 对溴苯甲酸甲酯 | CAS号171364-80-0 4-甲氧羰基苯硼酸频哪醇酯

📜4-甲氧甲酰苯硼酸频哪醇酯置于四(三苯基膦)钯,Lithium Hydroxide Monohydrate,Potassium Carbonate体系中,用 四氢呋喃,甲醇,乙醇,水,甲苯 用作溶剂,化学反应 10.0H,反应生成4-(5-硝基吡啶-2-基)苯甲酸
参考文献:Exploration Of Pyridine Containing Heteroaryl Analogs Of Biaryl Ureas As Dgat1 Inhibitors
标题:Exploration Of Pyridine Containing Heteroaryl Analogs Of Biaryl Ureas As Dgat1 Inhibitors
摘要:The Diacylglycerol Acyltransferase Enzyme,Dgat1,Presents Itself As A Potential Target For Obesity As This Enzyme Is Dedicated To The Final Committed Step In Triglyceride Biosynthesis. Biphenyl Ureas,Exemplified By Compound 4,Have Been Reported To Be Potent Hdgat1 Inhibitors. We Have Synthesized And Evaluated 2-Pyridyl And 3-Pyridyl Containing Biaryl Ureas As Hdgat1 Inhibitors. Our Aim Was To Incorporate A Heteroaryl Scaffold Within These Molecules Thereby Improving The C Log P Profile And Making These Compounds More Drug-Like. Compounds Within This Series Exhibited Potent Hdgat1 Inhibition When Evaluated Using An In Vitro Enzymatic Assay. Selected Compounds Were Also Subjected To An Oral Fat Tolerance Test In Mice Where The Percent Triglyceride Reduction Versus A Vehicle Control Was Evaluated. Of The Studied Heteroaryl Analogs Compound 44 Exhibited An In Vitro Ic50 Of 17 Nm And A Plasma Triglyceride Reduction Of 79% Along With A 12-Fold Improvement In Solubility Over The Biphenyl Urea Compound 4. (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2011.07.109