N-[5-(4-fluorophenoxy)-2-thienyl]methanesulphonamide

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-[5-(4-fluorophenoxy)-2-thienyl]methanesulphonamide
• 英文别名: RWJ 63556；N-[5-(4-fluorophenoxy)thiophen-2-yl]methanesulfonamide
• 化学式: C₁₁H₁₀FNO₃S₂
• 分子量: 287.336
• InChiKey: BEIZIEZPGSIQGR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  92
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-Nitro-5(4-fluoro)phenoxythiophene 在 ammonium hydroxide 、 铁粉 、 溶剂黄146 、 lithium diisopropyl amide 作用下， 以 甲醇 为溶剂， 反应 6.75h， 生成 N-[5-(4-fluorophenoxy)-2-thienyl]methanesulphonamide
  参考文献：
  名称：

  N-(5-substituted) thiophene-2-alkylsulfonamides as potent inhibitors of 5-lipoxygenase

  摘要：

  Compound 4k N-[5-(4-fluoro) phenoxythien-2-yl] methanesulfonamide is representative of a new class of potent inhibitors of 5-lipoxygenase (5-LO). These versatile compounds exhibit dose-dependent inhibition of 5-LO with IC(50)s ranging from 20-100 nM in the rat basophilic leukemia (RBL-1) cell homogenate assay and submicromolar IC,,s in both the RBL-1 and human peripheral blood leukocyte (PBL) whole cell assays. Compound 4k also showed significant anti-inflammatory activity in the adjuvant arthritic rat at an oral dose of 3 mg/kg. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0968-0896(97)00025-4

文献信息

• [DE] ARYLOXIME<br/>[EN] ARYLOXIMES<br/>[FR] ARYLOXYMES
  申请人：MERCK PATENT GMBH

  公开号：WO2003104205A1

  公开（公告）日：2003-12-18

  Aryloximderivate der Formel (I), worin R1, R2, R3, X und B die in Anspruch 1 angegebenen Bedeutungen haben, wirken als Phosphodiesterase IV-Inhibitoren und lassen sich zur Behandlung von Osteoporose, Tumoren, Kachexie, Atherosklerose, rheumatoider Arthritis, multipler Sklerose, Diabetes mellitus, entzündlichen Prozessen, Allergien, Asthma, Autoimmunkrankheiten, Myokarderkrankungen und AIDS einsetzen.

  Aryloximderivate der Formel (I), worin R1, R2, R3, X und B die in Anspruch 1 angegebenen Bedeutungen haben, wirken als Phosphodiesterase IV-Inhibitoren und lassen sich zur Behandlung von Osteoporose, Tumoren, Kachexie, Atherosklerose, rheumatoider Arthritis, multipler Sklerose, Diabetes mellitus, entzündlichen Prozessen, Allergien, Asthma, Autoimmunkrankheiten, Myokarderkrankungen und AIDS einsetzen.
• PYRIDAZINDERIVATE
  申请人：Merck Patent GmbH

  公开号：EP1509506B1

  公开（公告）日：2009-08-05
• ARYLOXIME
  申请人：Merck Patent GmbH

  公开号：EP1511737B1

  公开（公告）日：2010-02-17
• NOVEL COMPOSITION
  申请人：Chen Chien-Hung

  公开号：US20110281829A1

  公开（公告）日：2011-11-17

  This disclosure relates to a pharmaceutical composition that includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5′-monophosphate-activated protein kinase (AMPK) activator; a second agent that possesses anti-inflammatory activity; and a third agent that is a serotonin metabolite.
• NOVEL COMPOSITION FOR TREATING METABOLIC SYNDROME AND OTHER CONDITIONS
  申请人：Chen Chien-Hung

  公开号：US20120183600A1

  公开（公告）日：2012-07-19

  The invention relates to a composition that includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5′-monophosphate-activated protein kinase (AMPK) activator; a second agent that possesses anti-inflammatory activity; and a third agent that possesses serotonin activity.