FG 1731

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: FG 1731
• 英文别名: N-Hydroxy-3-[(4-methoxyphenethyl)-(4-(3-benzyl-ureido)benzenesulfonyl)-amino]-propionamide；3-[[4-(benzylcarbamoylamino)phenyl]sulfonyl-[2-(4-methoxyphenyl)ethyl]amino]-N-hydroxypropanamide
• 化学式: C₂₆H₃₀N₄O₆S
• 分子量: 526.613
• InChiKey: RTOXIYMJLZFAIX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  37
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  145
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  4-(氯磺酰)异氰酸苯酯 在 羟胺 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 FG 1731
  参考文献：
  名称：

  Design and synthesis of procollagen C-proteinase inhibitors

  摘要：

  Non-peptidic inhibitors of procollagen C-proteinase (PCP) were designed from substrate leads. Compounds were optimized for potency and selectivity, with N-substituted aryl sulfonamide hydroxamates having the best combination of these properties. Compounds 89 and 60 have IC50 values of 10 and 80 nM, respectively, against PCP; excellent selectivity over MMP's 1, 2, and 9; and activity in cell-based collagen deposition assays. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.10.067

文献信息

• N-substituted arylsulfonylamino hydroxamic acids useful as inhibitors of C-proteinase and for treating or preventing disorders related to unregulated collagen production
  申请人：——

  公开号：US20030191309A1

  公开（公告）日：2003-10-09

  The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.

  本发明涉及一种新型有机分子类，能够抑制C-蛋白酶，并且利用它们来调节、调节和/或抑制异常胶原形成，作为治疗纤维化疾病的治疗方法。
• N-SUBSTITUTED ARYLSULFONYLAMINO HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF C-PROTEINASE AND FOR TREATING OR PREVENTING DISORDERS RELATED TO UNREGULATED COLLAGEN PRODUCTION
  申请人：FIBROGEN, INC.

  公开号：EP1154992A1

  公开（公告）日：2001-11-21
• EP1154992A4
  申请人：——

  公开号：EP1154992A4

  公开（公告）日：2003-05-28
• US6506936B1
  申请人：——

  公开号：US6506936B1

  公开（公告）日：2003-01-14
• [EN] N-SUBSTITUTED ARYLSULFONYLAMINO HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF C-PROTEINASE AND FOR TREATING OR PREVENTING DISORDERS RELATED TO UNREGULATED COLLAGEN PRODUCTION<br/>[FR] ACIDES HYDROXAMIQUES ARYLSULFONYLAMINES N-SUBSTITUES, INHIBITEURS DE PROTEASE C, ET TRAITANT OU PREVENANT DES TROUBLES LIES A LA PRODUCTION NON REGULEE DE COLLAGENE
  申请人：FIBROGEN INC

  公开号：WO2000050390A1

  公开（公告）日：2000-08-31

  The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.