N-benzyl-8-methoxyquinoline-5-sulfonamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N-benzyl-8-methoxyquinoline-5-sulfonamide
• 化学式: C₁₇H₁₆N₂O₃S
• mdl: MFCD03036157
• 分子量: 328.4
• InChiKey: UPPWEEIDGQQZNE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.117
• 拓扑面积：
  76.7
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  8-甲氧基-5-喹啉磺酰氯 、 苄胺 以36%的产率得到
  参考文献：
  名称：

  TOCHILKIN, A. I.;GRACHEVA, I. N., BIOORGAN. XIMIYA, 16,(1990) N, S. 956-962

  摘要：

  DOI：

文献信息

• QUINOLINE SULFONAMIDES AS TNF INHIBITORS AND AS PDE-IV INHIBITORS
  申请人：Darwin Discovery Limited

  公开号：EP0912519A1

  公开（公告）日：1999-05-06
• US5834485A
  申请人：——

  公开号：US5834485A

  公开（公告）日：1998-11-10
• [EN] QUINOLINE SULFONAMIDES AS TNF INHIBITORS AND AS PDE-IV INHIBITORS<br/>[FR] SULFONAMIDES DE QUINOLINE EN TANT QU'INHIBITEURS DE TNF ET INHIBITEURS DE PHOTODIESTERASE-IV
  申请人：DARWIN DISCOVERY LIMITED

  公开号：WO1997044322A1

  公开（公告）日：1997-11-27

  (EN) A compound of general formula (i), wherein R is H, halogen or alkyl; R1 represents OH, alkoxy optionally substituted with one or more halogens, or thioalkyl; R2, R3 and R4 are the same or different and are each H, R7, OR11, COR7, C(=NOR7)R7, alkyl-C(=NOR7)R7, alkyl-C(=NOH)R7, C(=NOH)R7, halogen, CF3, CN, CO2H, CO2R11, CONH2, CONHR7, CON(R7)2, NR9R10 or CONR12R13 where NR12R13 is a heterocyclic ring optionally substituted with one or more R15; R5 represents H, arylalkyl, heteroarylalkyl, S(O)mR11 or alkyl optionally substituted with one or more substituents chosen from hydroxy, alkoxy, CO2R8, SO2NR12R13, CONR12R13, CN, carbonyl oxygen, NR9R10, COR11 and S(O)nR11; R6 represents aryl, heteroaryl, arylalkyl or heteroarylalkyl. The compounds can be used to treat disease states, for example disease states associated with proteins that mediate cellular activity, for example by inhibiting tumour necrosis factor and/or by inhibiting phosphodiesterase IV.(FR) Composé de formule générale (i) dans laquelle R est H, halogène ou alkyle; R1 représente OH, alcoxy éventuellement substitué par un ou plusieurs halogènes, ou thioalkyle; R2, R3 et R4 sont identiques ou différents et sont chacun H, R7, OR11, COR7, C(=NOR7)R7, alkyl-C(=NOR7)R7, alkyl-C(=NOH)R7, C(=NOH)R7, halogène, CF3, CN, CO2H, CO2R11, CONH2, CONHR7, CON(R7)2, NR9R10 ou CONR12R13 dans laquelle NR12R13 est un noyau hétérocyclique éventuellement substitué par un ou plusieurs R15; R5 est H, arylalkyle, hétéroarylalkyle, S(O)mR11 ou alkyle éventuellement substitué par un ou plusieurs substituants choisi parmi hydroxy, alcoxy, CO2R8, SO2NR12R13, CON12R13, CN, oxygène carbonyle, NR9R10, COR11 et S(O)nR11; R6 est aryle, hétéroaryle, arylalkyle ou hétéroarylalkyle. Lesdits composés peuvent être utilisés pour traiter des maladies, telles des états pathologiques associés aux protéines qui induisent l'activité cellulaire, par exemple en inhibant le facteur de nécrose tumorale (TNF) et/ou en inhibant la photodiestérase-IV.
• [EN] KINASE INHIBITORS CAPABLE OF INCREASING THE SENSITIVITY OF BACTERIAL PATHOGENS TO B-LACTAM ANTIBIOTICS<br/>[FR] INHIBITEURS DE KINASES CAPABLES DE RENFORCER LA SENSIBILITÉ D'AGENTS PATHOGÈNES BACTÉRIENS AUX ANTIBIOTIQUES DE LA FAMILLE DES B-LACTAMINES
  申请人：SEATTLE CHILDREN S RES INST

  公开号：WO2013066469A2

  公开（公告）日：2013-05-10

  Staphylococcus aureus are gram-positive bacteria that are currently the leading cause of invasive infections in humans. While antibiotic therapy is currently used to treat S. aureus infections, the emergence of antibiotic resistant strains such as those resistant to methicillan are rapidly exhausting treatment options. Disclosed herein are methods and compositions for increasing the sensitivity of bacterial pathogens to β-lactam antibiotics. Also disclosed herein are genes involved in modulating antibiotic resistance which serve as novel targets for treatments aimed at inhibiting antibiotic resistant bacterial pathogens. Also disclosed herein are kinase inhibitors which demonstrate superior activity in sensitizing bacterial pathogens to β-lactam antibiotics.
• TOCHILKIN, A. I.;GRACHEVA, I. N., BIOORGAN. XIMIYA, 16,(1990) N, S. 956-962
  作者：TOCHILKIN, A. I.、GRACHEVA, I. N.

  DOI：——

  日期：——