CAS: 190774-58-4; 2,3,4-Trifluorophenylisocyanate

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phosgene 2,3,4-trifluoroaniline 1-(2-hydroxy-4-nitrophenyl)-3-(2,3,4-trifluorophenyl)urea 2-adamantyl 2,3,4-trifluorophenylcarbamate 1-((6,6-dimethylbicyclo[3.1.1]heptan-2-yl)methyl)-3-(2,3,4-trifluorophenyl)urea 1-(2,3,4-trifluorophenyl)-3-(2,6,6-trimethylbicyclo[3.1.1]heptan-3-yl)urea

📜光气,2,3,4-三氟苯胺置于碳酸氢钠体系中,用 二氯甲烷,水,甲苯 用作溶剂,化学反应生成2,3,4-三氟苯基异氰酸酯
参考文献:Structural Optimization Of A Cxcr2-Directed Antagonist That Indirectly Inhibits γ-Secretase And Reduces Aβ
标题:Structural Optimization Of A Cxcr2-Directed Antagonist That Indirectly Inhibits γ-Secretase And Reduces Aβ
摘要:Amyloid Beta(A Beta),A Key Molecule In The Pathogenesis Of Alzheimer'S Disease (Ad),Is Derived From The Amyloid Precursor Protein (App) By Sequential Proteolysis Via Beta-And Gamma-Secretases. Because Of Their Role In Generation Of A Beta,These Enzymes Have Emerged As Important Therapeutic Targets For Ad. In The Case Of Gamma-Secretase,Progress Has Been Made Towards Designing Potent Inhibitors With Suitable Pharmacological Profiles. Direct Gamma-Secretase Inhibitors Are Being Evaluated In Clinical Trials And New Strategies Are Being Explored To Block Gamma-Secretase Activity Indirectly As Well. In This Regard,We Have Previously Reported An Indirect Regulation Of Gamma-Secretase Through Antagonism Of Cxcr2,A G-Protein Coupled Receptor (Gpcr). We Demonstrated That N-(2-Hydroxy-4-Nitrophenyl)-N'-(2-Bromophenyl)Urea (Sb225002),A Selective Inhibitor Of Cxcr2 Also Plays A Role In An Indirect Inhibition Of Gamma-Secretase. Furthermore,We Reported A Similar To 5-Fold Difference In The Selective Inhibition Of App Versus Notch Processing Via Gamma-Secretase Following Treatment With Sb225002. Herein We Describe The Synthesis And Optimization Of Sb225002. By Determination Of The Structure-Activity Relationship (Sar),We Derived Small Molecules That Inhibit A Beta 40 Production With Ic(50) Values In The Sub-Micromolar Range In A Cell-Based Assay And Also Validated The Potential Of Cxcr2 As A New Target For Therapeutic Intervention In Ad. (C) 2009 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2009.09.051