Glycine [(5R)-3-[3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl ester | 856866-74-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Glycine [(5R)-3-[3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl ester
• 英文别名: [(5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl 2-aminoacetate
• CAS: 856866-74-5
• 化学式: C₁₉H₁₈FN₇O₄
• 分子量: 427.4
• InChiKey: AIKIAPJCJGCCSZ-CYBMUJFWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  138
• 氢给体数：
  1
• 氢受体数：
  10

文献信息

• Novel oxazolidinone derivatives
  申请人：Rhee Keol Jae

  公开号：US20070155798A1

  公开（公告）日：2007-07-05

  The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium . Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic. Data supplied from the esp@cenet database—Worldwide

  本发明涉及一种新型的噁唑烷酮衍生物及其制备方法和含有该衍生物的药物组合物，用于抗生素。本发明的噁唑烷酮衍生物对广谱细菌具有抑制活性，且毒性较低。通过将具有羟基的化合物与氨基酸或磷酸反应制备的前药，在溶解性方面具有优异的效率。此外，本发明的衍生物可能对各种人类和动物病原体具有强效的抗菌活性，包括革兰氏阳性菌，如葡萄球菌、肠球菌和链球菌，厌氧微生物，如拟杆菌和梭状芽孢杆菌，以及耐酸微生物，如结核分枝杆菌和鸟型分枝杆菌。因此，含有噁唑烷酮的组合物用于抗生素。数据来源于esp@cenet数据库-全球。
• NOVEL OXAZOLIDINONE DERIVATIVES
  申请人：DONG-A ST CO., LTD.

  公开号：US20130281492A1

  公开（公告）日：2013-10-24

  The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi , anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium . Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

  本发明涉及新型的噁唑烷酮衍生物及其制备方法和包含该衍生物的药物组合物，用于抗生素。本发明的噁唑烷酮衍生物显示出对广谱细菌的抑制活性和较低的毒性。通过将具有羟基的化合物与氨基酸或磷酸反应制备的前药，在水中的溶解度具有极高的效率。此外，本发明的衍生物可能对各种人类和动物病原体具有强效的抗菌活性，包括革兰氏阳性菌，如葡萄球菌，肠球菌和链球菌，厌氧微生物，如拟杆菌和梭菌，以及耐酸微生物，如结核分枝杆菌和埃希氏菌。因此，包含噁唑烷酮的组合物用于抗生素。
• EP1699784B1
  申请人：——

  公开号：EP1699784B1

  公开（公告）日：2011-06-29
• THERAPEUTIC COMBINATION OF DAPTOMYCIN AND PROTEIN SYNTHESIS INHIBITOR ANTIBIOTIC, AND METHODS OF USE
  申请人：Trius Therapeutics, Inc.

  公开号：US20130102523A1

  公开（公告）日：2013-04-25

  A therapeutic combination comprises an antibacterially effective amount of daptomycin, and an amount of protein synthesis inhibitor antibiotic effective to prevent the development of daptomycin non-susceptibility in bacteria. Related combination therapies and methods are also included.
• US7816379B2
  申请人：——

  公开号：US7816379B2

  公开（公告）日：2010-10-19