5,6-Dihydro-8(7H)-chinolinonoximo-p-toluolsulfonat | 67046-21-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5,6-Dihydro-8(7H)-chinolinonoximo-p-toluolsulfonat
• 英文别名: O-tosyl-6,7-dihydroquinolin-8(5H)-one oxime；(6,7-dihydro-5H-quinolin-8-ylideneamino) 4-methylbenzenesulfonate
• CAS: 67046-21-3
• 化学式: C₁₆H₁₆N₂O₃S
• 分子量: 316.381
• InChiKey: XEELHBIHPRUFFK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  77
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  (E)-6,7-二氢喹啉-8(5H)-酮肟 、 对甲苯磺酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 12.0h， 以78%的产率得到5,6-Dihydro-8(7H)-chinolinonoximo-p-toluolsulfonat
  参考文献：
  名称：

  WO2007/67416

  摘要：

  公开号：

文献信息

• [EN] ALKYLIDINE SUBSTITUTED HETEROCYCLYL DERIVATIVES AS ANTI-BACTERIAL AGENTS<br/>[FR] DÉRIVÉS D'HÉTÉROCYCLYL SUBSTITUÉS PAR ALKYLIDINE COMME AGENTS ANTIBACTÉRIENS
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2015071780A1

  公开（公告）日：2015-05-21

  The present invention relates to alkylidine substituted heterocyclyl derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors; I in which P, Q, Ri, R2, R3 and "n" have the same meanings given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FABI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明涉及公式（1）的烷基亚甲基取代的杂环衍生物，其可能作为抗菌剂在治疗上有用，更具体地是FAbI抑制剂;其中P，Q，Ri，R2，R3和“n”具有规范中给出的相同含义，并且其药学上可接受的盐或药学上可接受的立体异构体在疾病或紊乱的治疗和预防中有用，特别是在抑制乙酰辅酶A还原酶酶（FABI）活性方面具有优势的疾病或紊乱的使用。本发明还提供合成和给予FAbI抑制剂化合物的方法。本发明还提供包含至少一种FAbI抑制剂化合物的药物制剂，以及其药学上可接受的载体，稀释剂或赋形剂。
• 3-Heterocyclylacrylamide Compounds as Fab I Inhibitors and Antibacterial Agents
  申请人：Pauls Henry

  公开号：US20090156578A1

  公开（公告）日：2009-06-18

  In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.

  本发明的部分涉及具有FabI抑制性质的化合物。这些化合物也可能抑制其他酶，包括那些在结构或功能上类似于FabI的酶，例如Fab K。还提供了包括所述化合物的试剂盒和组合物。还揭示了治疗细菌性疾病患者的方法。
• 3-HETEROCYCLYLACRYLAMIDE COMPOUNDS AS FABI INHIBITORS AND ANTIBACTERIAL AGENTS
  申请人：Affinium Pharmaceuticals, Inc.

  公开号：EP1973902A2

  公开（公告）日：2008-10-01
• US20140275019A1
  申请人：——

  公开号：US20140275019A1

  公开（公告）日：2014-09-18
• [EN] THERAPEUTIC AGENTS, AND METHODS OF MAKING AND USING THE SAME<br/>[FR] AGENTS THERAPEUTIQUES ET SES PROCÉDÉS DE FABRICATION ET D'UTILISATION
  申请人：AFFINIUM PHARM INC

  公开号：WO2007067416A2

  公开（公告）日：2007-06-14

  [EN] In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.
  [FR] La présente invention concerne en partie des composés possédant des propriétés d'inhibition FabI. De tels composés peuvent aussi inhiber d'autres enzymes, dont ceux similaires à FabI soit structurellement soit fonctionnellement, par exemple, Fab K. Sont également fournis des kits et des compositions qui incluent les composés présentés. L'invention concerne aussi des procédés de traitement d'un sujet souffrant d'une infection bactérienne.