N-(3-methylisoxazol-5-yl)methoxyphthalimide | 156233-48-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: N-(3-methylisoxazol-5-yl)methoxyphthalimide
• 英文别名: 2-[(3-methyl-1,2-oxazol-5-yl)methoxy]isoindole-1,3-dione
• CAS: 156233-48-6
• 化学式: C₁₃H₁₀N₂O₄
• 分子量: 258.233
• InChiKey: XEQKYEJIQDCLCK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  72.6
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-(3-methylisoxazol-5-yl)methoxyphthalimide 在 盐酸 、 一水合肼 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 2.0h， 生成 (2S,3R,5R)-3-Methyl-3-[(3-methyl-isoxazol-5-ylmethoxyimino)-methyl]-4,4,7-trioxo-4λ⁶-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid 4-methoxy-benzyl ester
  参考文献：
  名称：

  Synthesis and Evaluation of 2β-0xyimino and Alkenylpenicillanic Acid Sulfone Derivatives as β-Lactamase Inhibitors

  摘要：

  The synthesis and in vitro synergies of 2 beta-alkenyl and oxyiminopenam sulfone derivatives are described. Most of the compounds synthesized exhibited good inhibitory activities and synergistic antibacterial activities with piperacillin and ceftriaxone, respectively, against several beta-lactamase producing strains. Particularly the 2 beta-alkenylpenam sulfone derivatives. 1e and 1g, showed good synergistic activity with ceftriaxone against Citrobacter freundi NIH 10018-68 and Proteus vulgaris 20. Also the compounds 2a, 2c, and 2f, 2 beta-oxyiminopenam sulfone derivatives, exhibited improved synergistic activity with piperacillin against Citrobacter freundi NIH 10018-68.

  DOI：

  10.1002/(sici)1521-4184(19991)332:1<7::aid-ardp7>3.0.co;2-m
• 作为产物：
  描述：

  N-(isoxazol-4-yl)methoxyphthalimide 、 四羟甲基异恶唑 生成 N-(3-methylisoxazol-5-yl)methoxyphthalimide
  参考文献：
  名称：

  Octahydronaphthalene oxime derivatives for cholesterol biosynthesis

  摘要：

  式(I)的化合物：##STR1## （其中：R为氢，甲基或羟基；X为烷基，烯基，环烷基，芳基，芳基烷基或杂环基；A为单键，或烷基，烯基，炔基或烯炔基；Y为氢，芳基，环烷基或杂环基）具有抑制胆固醇生物合成的能力，因此可用于治疗和预防与高血胆固醇水平有关的疾病。

  公开号：

  US05604256A1

文献信息

• Octahydronaphthalene oxime derivatives for cholesterol biosynthesis inhibition, their preparation and use
  申请人：SANKYO COMPANY LIMITED

  公开号：EP0570245A2

  公开（公告）日：1993-11-18

  Compounds of formula (I) : (in which: R is hydrogen, methyl or hydroxy; X is alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or a heterocyclic group; A is a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y is hydrogen, aryl, cycloalkyl or a heterocyclic group) have the ability to inhibit the biosynthesis of cholesterol, and can thus be used for the treatment and prophylaxis of diseases relating to high blood cholesterol levels.

  式(I)化合物： 其中R为氢、甲基或羟基；X为烷基、烯基、环烷基、芳基、芳烷基或杂环基；A为单键或亚烷基、亚烯基、亚炔基或烷二烯基；Y为氢、芳基、环烷基或杂环基）具有抑制胆固醇生物合成的能力，因此可用于治疗和预防与高血胆固醇水平有关的疾病。
• TRICYCLIC COMPOUND HAVING SULFINYL OR SULFONYL
  申请人：Shionogi & Co., Ltd.

  公开号：US20180186814A1

  公开（公告）日：2018-07-05

  The present invention provides a compound exhibiting a strong antimicrobial spectrum against various bacteria, including gram-negative bacteria, or a pharmaceutical composition having an antimicrobial activity carbapenem-resistant bacteria. Provided is a compound represented by formula (I), an ester thereof or a pharmaceutically acceptable salt thereof, or a hydrate thereof. (I) (in the formula, —W— is —S(═O)— or S(═O) 2 —, -T- is CR 4A R 4B — or —CR 5A —R 5B —CR 6A —R 6B —, each of R 2A and R 2B is independently a hydrogen atom, etc., or R 2A and R 2B together form a substituted or unsubstituted methylidene, etc., R 3 is a hydrogran atom, etc., R 11 is a carboxyl, etc., and each of R 7A and R 7B is independently a hydrogen atom, etc.)
• US5604256A
  申请人：——

  公开号：US5604256A

  公开（公告）日：1997-02-18
• Synthesis and Evaluation of 2β-0xyimino and Alkenylpenicillanic Acid Sulfone Derivatives as β-Lactamase Inhibitors
  作者：Young Seo Cho、Young Jin Ha、Jin Sun Kwon、Ae Nim Pae、Kyung Il Choi、Hun Yeong Koh、Moon Ho Chang、Cheol-Min Yoon、Gwan Sun Lee

  DOI：10.1002/(sici)1521-4184(19991)332:1<7::aid-ardp7>3.0.co;2-m

  日期：1999.1

  The synthesis and in vitro synergies of 2 beta-alkenyl and oxyiminopenam sulfone derivatives are described. Most of the compounds synthesized exhibited good inhibitory activities and synergistic antibacterial activities with piperacillin and ceftriaxone, respectively, against several beta-lactamase producing strains. Particularly the 2 beta-alkenylpenam sulfone derivatives. 1e and 1g, showed good synergistic activity with ceftriaxone against Citrobacter freundi NIH 10018-68 and Proteus vulgaris 20. Also the compounds 2a, 2c, and 2f, 2 beta-oxyiminopenam sulfone derivatives, exhibited improved synergistic activity with piperacillin against Citrobacter freundi NIH 10018-68.
• Octahydronaphthalene oxime derivatives for cholesterol biosynthesis
  申请人：Sankyo Company, Limited

  公开号：US05604256A1

  公开（公告）日：1997-02-18

  Compounds of formula (I): ##STR1## (in which: R is hydrogen, methyl or hydroxy; X is alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or a heterocyclic group; A is a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y is hydrogen, aryl, cycloalkyl or a heterocyclic group) have the ability to inhibit the biosynthesis of cholesterol, and can thus be used for the treatment and prophylaxis of diseases relating to high blood cholesterol levels.

  式(I)的化合物：##STR1## （其中：R为氢，甲基或羟基；X为烷基，烯基，环烷基，芳基，芳基烷基或杂环基；A为单键，或烷基，烯基，炔基或烯炔基；Y为氢，芳基，环烷基或杂环基）具有抑制胆固醇生物合成的能力，因此可用于治疗和预防与高血胆固醇水平有关的疾病。