| 1399360-39-4

• 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
• CAS: 1399360-39-4
• 化学式: C₁₅H₃₁N₃O₃
• 分子量: 301.429
• InChiKey: LPRICCDKQKCJQJ-GFCCVEGCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  21.0
• 可旋转键数：
  7.0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.87
• 拓扑面积：
  70.67
• 氢给体数：
  2.0
• 氢受体数：
  4.0

反应信息

• 作为反应物：
  描述：

  在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 反应 1.0h， 生成 (2R)-2-amino-N-[3-(dimethylamino)propyl]-3-methylbutanamide
  参考文献：
  名称：

  Antiparasitic activities of novel, orally available fumagillin analogs

  摘要：

  Fumagillin, an irreversible inhibitor of MetAP2, has been shown to potently inhibit growth of malaria parasites in vitro. Here, we demonstrate activity of fumagillin analogs with an improved pharmacokinetic profile against malaria parasites, trypanosomes, and amoebas. A subset of the compounds showed efficacy in a murine malaria model. The observed SAR forms a basis for further optimization of fumagillin based inhibitors against parasitic targets by inhibition of MetAP2. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.07.029
• 作为产物：
  描述：

  N,N-二甲基-1,3-二氨基丙烷 生成
  参考文献：
  名称：

  Antiparasitic activities of novel, orally available fumagillin analogs

  摘要：

  Fumagillin, an irreversible inhibitor of MetAP2, has been shown to potently inhibit growth of malaria parasites in vitro. Here, we demonstrate activity of fumagillin analogs with an improved pharmacokinetic profile against malaria parasites, trypanosomes, and amoebas. A subset of the compounds showed efficacy in a murine malaria model. The observed SAR forms a basis for further optimization of fumagillin based inhibitors against parasitic targets by inhibition of MetAP2. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.07.029

文献信息

• [EN] OXASPIRO [2.5] OCTANE DERIVATIVES AND ANALOGS<br/>[FR] DÉRIVÉS D'OXASPIRO[2.5]OCTANE ET ANALOGUES
  申请人：ZAFGEN CORP

  公开号：WO2012122264A1

  公开（公告）日：2012-09-13

  The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity.

  这项发明提供了氧杂螺[2.5]辛烷衍生物和类似物，其制备方法，中间体，药物组合物以及在治疗各种疾病和状况中的用途，例如超重和肥胖。