CAS: 586379-66-0; 3-(3-Bromo-4-((2,4-Difluorobenzyl)Oxy)-6-Methyl-2-Oxopyridin-1(2H)-yl)-N,4-Dimethylbenzamide
该化合物是其潜在的治疗用途,被归类为小分子,并被视为某些蛋白性动脉的选择性抑制剂,这些蛋白性酶在各种细胞信号路径中至关重要.该化合物的结构通常具有核心特征,允许与目标蛋白进行特定互动,有助于其生物活动.PH 797804已经研究过它对细胞扩散和流行性中毒的影响,使其成为癌症研究的候选对象.此外,其药用植物基因特性,例如溶性与稳定性,对于确定临床环境的功效和安全性至关重要.与许多调查性化合物一样,正在进行的研究旨在阐明其行动机制,最佳剂量疗程和潜在副作用.
- 英文名称3-(3-Bromo-4-((2,4-Difluorobenzyl)Oxy)-6-Methyl-2-Oxopyridin-1(2H)-yl)-N,4-Dimethylbenzamide
- 中文名称3-溴-4-(2,4-二氟苄氧基)-1-[5-[(甲基氨基)羰基]-2-甲基苯基]-6-甲基吡啶-2(1H)-酮
- IUPAC名称3-(3-bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide
- 其它别名3-(3-Bromo-4-((2,4-Difluorobenzyl)Oxy)-6-Methyl-2-Oxopyridin-1(2H)-yl)-N,4-Dimethylbenzamide
- CAS编号586379-66-0
- MFCD编号:MFCD18251426
- EINECS号:110-020-2
- 分子式:C22H19BrF2N2O3分子量:477.3
- 产品CID: 1561358
- 产品分类生物化工 → 抑制剂 → 丝裂原活化蛋白激酶(MAPK)
物理性质
- 沸点593.2±50.0 °C at 760 mmHg
- 闪点312.6±30.1 °C
- 密度1.5±0.1 g/cm3
- PSA:60.33
- LogP:3.24
- 折射率1.629
- 蒸汽压0.0±1.7 mmHg at 25°C
- 溶解性≥23.85 mg/mL In DMSO; Insoluble In H2O; Insoluble In Etoh
- 外观形态白色至米色粉末
- 储存条件20-25°C
- 产品应用该化合物是一种新颖的,基于丙烯酮的P38Α抑制剂,具有很强的抗炎活动;它有效抑制了LPS引起的TNF-Α生产以及人类单体U937细胞中的38个流动酶活动(分别为IC50=5.9 NM和1.1 NM);它以依赖浓度的方式抑制了主要大鼠骨髓髓髓细胞中的RANKL-和M-CSF引起的骨血管形成(IC50 = 3 NM);它显示出对P38FFE的抑制剂高选择性性,超过其他血管细胞的强性(CDK2, IRK2, IRG1, IKKK02, IKOKI,MAPKAP2,MAMAKAP3, MKK7 (>100 ΜM), MNKK,MSK (>164 MILM), PRAK,RSK 2 和TBK1);它通过口服,对PH-7904的口服对由大鼠内和辛基猴内内内分泌的异丙猴引发的急性急性急性反应的急性反应,它能性抗药性能.
MSDS等安全信息
欧盟法规
C&L通报上下游产品
methylamine 4-hydroxy-6-methyl-2-pyron methyl 3-(4-hydroxy-6-methyl-2-oxopyridin-1(2H)-yl)-4-methylbenzoate 3-(5-bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1(2H)-yl)-4-methylbenzoic acid(-)-3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide合成工艺路线路线简述
📜Methyl 3-(4-Hydroxy-6-Methyl-2-Oxopyridin-1(2H)-yl)-4-Methylbenzoate置于溴,Potassium Carbonate,1-羟基苯并三唑,溶剂黄146,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,Lithium Hydroxide体系中,用 四氢呋喃,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 3-溴-4-(2,4-二氟苄氧基)-1-[5-[(甲基氨基)羰基]-2-甲基苯基]-6-甲基吡啶-2(1H)-酮
参考文献:Discovery Of Ph-797804,A Highly Selective And Potent Inhibitor Of P38 Map Kinase
标题:Discovery Of Ph-797804,A Highly Selective And Potent Inhibitor Of P38 Map Kinase
摘要:The Synthesis And Sar Studies Of A Novel N-Aryl Pyridinone Class Of P38 Kinase Inhibitors Are Described. Systematic Structural Modifications To The Hts Lead,5,Led To The Identification Of (-)-4A As A Clinical Candidate For The Treatment Of Inflammatory Diseases. Additionally,The Chiral Synthesis And Properties Of (-)-4A Are Described. (C) 2011 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2011.04.121
海关参考信息
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2912110000-甲醛
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