2-[3,5-Dimethyl-4-hydroxy(phenyl)]-4-(4-fluorophenyl)-5-(4-pyridyl)-1H-imidazole | 152121-43-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-[3,5-Dimethyl-4-hydroxy(phenyl)]-4-(4-fluorophenyl)-5-(4-pyridyl)-1H-imidazole
• 英文别名: 2-[3,5-Dimethyl-4-hydroxy(phenyl)]-4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazole；4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]-2,6-dimethyl-phenol；4-[4-(4-fluorophenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]-2,6-dimethylphenol
• CAS: 152121-43-2
• 化学式: C₂₂H₁₈FN₃O
• 分子量: 359.403
• InChiKey: TZQNFQCZKXEYMY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  61.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• POTENTIATORS OF BETA-LACTAM ANTIBIOTICS
  申请人：UNIVERSITY OF NOTRE DAME DU LAC

  公开号：US20180044316A1

  公开（公告）日：2018-02-15

  We disclose herein that the BlaR1 protein of methicillin-resistant Staphylococcus aureus (MRSA), an antibiotic sensor/signal transducer, is phosphorylated on exposure to β-lactam antibiotics. This event is critical for the onset of the biochemical events that unleash induction of antibiotic resistance. The BlaR1 phosphorylation and the antibiotic-resistance phenotype are abrogated in the presence of inhibitors described herein that restore susceptibility of the organism to β-lactam antibiotics. The invention thus provides compounds and methods for abrogating antibiotic resistance to β-lactam antibiotics and for treating infections causes by antibiotics prone to developing resistance.

  我们在此披露，甲氧西林耐药金黄色葡萄球菌（MRSA）的BlaR1蛋白质是一种抗生素感受器/信号转导器，当暴露于β-内酰胺类抗生素时，该蛋白质被磷酸化。这一事件对于引发生物化学事件并释放抗生素耐药性的发生至关重要。BlaR1的磷酸化和抗生素耐药表型在存在本文所述的抑制剂时被废除，这些抑制剂恢复了该生物对β-内酰胺类抗生素的敏感性。因此，本发明提供了用于废除β-内酰胺类抗生素的抗生素耐药性和治疗由易于产生耐药性的抗生素引起的感染的化合物和方法。
• Novel compounds
  申请人：SmithKline Beecham Corporation

  公开号：US20030064997A1

  公开（公告）日：2003-04-03

  Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.

  小说2,4,5-三芳基咪唑化合物及其在治疗中的应用组成物。
• Combination therapy for treating, preventing or managing proliferative disorders and cancers
  申请人：——

  公开号：US20040067953A1

  公开（公告）日：2004-04-08

  The present invention relates to methods and compositions designed for the treatment, management or prevention of cancer. The methods of the invention comprise the administration of an effective amount of one or more inhibitors of JNK in combination with the administration of an effective amount of one or more other agents useful for cancer therapy. The invention also provides pharmaceutical compositions comprising one or more inhibitors of JNK in combination with one or more other agents useful for cancer therapy. In particular, the invention is directed to methods of treatment and prevention of cancer by the administration of an effective amount of one or more inhibitors of JNK in combination with standard and experimental chemotherapies, hormonal therapies, bone marrow transplants, stem cell replacement therapies, biological therapies/immunotherapies and/or radiation therapies for treatment or prevention of cancer. Also included are methods of treatment of cancer by the administration of one or more inhibitors of JNK in combination with surgery, alone or in further combination with standard and experimental chemotherapies, hormonal therapies, bone marrow transplants, stem cell replacement therapies, biological therapies/immunotherapies and/or radiation therapies.

  本发明涉及用于治疗、控制或预防癌症的方法和组合物。本发明的方法包括施用有效量的一种或多种 JNK 抑制剂，并结合施用有效量的一种或多种其他用于癌症治疗的制剂。本发明还提供了药物组合物，其中包含一种或多种 JNK 抑制剂与一种或多种其他有助于癌症治疗的药物。特别是，本发明涉及通过施用有效量的一种或多种JNK抑制剂与标准和实验性化疗、激素疗法、骨髓移植、干细胞替代疗法、生物疗法/免疫疗法和/或放射疗法联合治疗或预防癌症的方法。还包括通过施用一种或多种JNK抑制剂结合手术、单独或进一步结合标准和实验性化疗、激素疗法、骨髓移植、干细胞替代疗法、生物疗法/免疫疗法和/或放射疗法治疗癌症的方法。
• COMBINATION THERAPY FOR TREATING, PREVENTING OR MANAGING PROLIFERATIVE DISORDERS AND CANCERS
  申请人：Signal Pharmaceuticals, Inc.

  公开号：EP1487436A1

  公开（公告）日：2004-12-22
• EP1487436A4
  申请人：——

  公开号：EP1487436A4

  公开（公告）日：2009-06-03