3-O-去克拉定糖红霉素肟 | 189108-61-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 3-O-去克拉定糖红霉素肟
• 英文名称: (E)-5-O-desosaminylerythronolide A 9-oxime
• 英文别名: (3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-4,7,12,13-tetrahydroxy-10-hydroxyimino-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one
• CAS: 189108-61-0
• 化学式: C₂₉H₅₄N₂O₁₀
• 分子量: 590.755
• InChiKey: YJRGIMSNCPMDGW-NRVYKBGMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  41
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.93
• 拓扑面积：
  182
• 氢给体数：
  6
• 氢受体数：
  12

反应信息

• 作为反应物：
  描述：

  3-O-去克拉定糖红霉素肟 在 三甲基乙酰氯 、 sodium carbonate 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 3.5h， 生成 (3R,4S,5S,6R,7R,9R,11S,12R,13S,14R,E)-6-(((2S,3R,4S,6R)-3-acetoxy-4-(dimethylamino)-6-methyltetrahydro-2H-pyran-2-yl)oxy)-10-(acetoxyimino)-14-ethyl-7,12,13-trihydroxy-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-4-yl 2-(pyridin-3-yl)acetate
  参考文献：
  名称：

  Synthesis and Antibacterial Activity of a Novel Series of Acylides:  3-O-(3-Pyridyl)acetylerythromycin A Derivatives

  摘要：

  A novel series of acylides, 3-O-(aryl)acetylerythromycin A derivatives, were synthesized and evaluated. These compounds have significant potent antibacterial activity against not only Gram-positive pathogens, including inducibly macrolide-lincosamide-streptogramin B (MLSB)-resistant and efflux-resistant strains, but also Gram-negative pathogens, such as H. influenzae. 6,9:11,12-Dicarbonate acylide 47 (FMA0122) was twice as active against H. influenzae than azithromycin, whereas it showed only moderate in vivo efficacy in mouse protection tests. However, the 11,12-carbamate acylide 19 (TEA0929), which showed potent antibacterial activity against almost all of the main causative pathogens of community-acquired pneumonia tested, exhibited excellent in vivo efficacy comparable to those of second-generation macrolides.

  DOI：

  10.1021/jm020568d
• 作为产物：
  描述：

  erythromycin A 9-(E)-oxime 在 盐酸 、 甲醇 、 水 、 potassium carbonate 作用下， 反应 3.0h， 生成 3-O-去克拉定糖红霉素肟
  参考文献：
  名称：

  WO2006/65721

  摘要：

  公开号：

文献信息

• C-9 ALKENYLIDINE BRIDGED MACROLIDES
  申请人：Phan Ly Tam

  公开号：US20080119418A1

  公开（公告）日：2008-05-22

  The present invention discloses compounds of formulae (I), (II) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

  本发明揭示了以下化合物的公式（I），（II）或其药学上可接受的盐，酯或前药：具有抗菌性质。本发明还涉及包括上述化合物的制药组合物，用于治疗需要抗生素治疗的受体。本发明还涉及通过给予包含本发明化合物的制药组合物来治疗受体的细菌感染的方法。本发明还包括制备本发明化合物的方法。
• 3,6-Bridged 9,12-oxolides
  申请人：Or Sun Yat

  公开号：US20070232554A1

  公开（公告）日：2007-10-04

  The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

  本发明揭示了公式（I）的化合物或其药学上可接受的盐、酯或前药：具有抗菌性能。本发明还涉及包含上述化合物的制药组合物，用于治疗需要抗生素治疗的受体。本发明还涉及通过给予包含本发明化合物的制药组合物来治疗受体的细菌感染的方法。本发明还包括制备本发明化合物的方法。
• WO2006/65721
  申请人：——

  公开号：——

  公开（公告）日：——
• WO2006/65743
  申请人：——

  公开号：——

  公开（公告）日：——
• US7291602B2
  申请人：——

  公开号：US7291602B2

  公开（公告）日：2007-11-06