2,6-dihydroxy-3-nitrobenzamide | 1129083-37-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: 2,6-dihydroxy-3-nitrobenzamide
• 英文别名: 2,6-Dihydroxy-5-nitrobenzamide
• CAS: 1129083-37-9
• 化学式: C₇H₆N₂O₅
• 分子量: 198.135
• InChiKey: YHFAUBOWOFLQCB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  129
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2,6-dihydroxy-3-nitrobenzamide 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 反应 18.0h， 以80%的产率得到3-amino-2,6-dihydroxybenzamide
  参考文献：
  名称：

  Bone selective effect of an estradiol conjugate with a novel tetracycline-derived bone-targeting agent

  摘要：

  In this study a novel bone-targeting agent containing elements of the tricarbonylmethane system of ring A of tetracycline was developed and was shown to bind to the mineral constituent of bone, hydroxyapatite. Conjugation of this bone-targeting agent to estradiol resulted in a bone-targeted estrogen (BTE2-A1) with an enhanced ability to bind to hydroxyapatite. In an ovariectomized rat model of osteoporosis a partial separation of the skeletal effects of estradiol from the uterine effects was observed following subcutaneous administration of BTE2-A1. This novel bone-targeting estradiol delivery system has the potential to improve the safety pro. le of estradiol in the treatment of osteoporosis. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.12.051
• 作为产物：
  描述：

  2,6-二羟基苯甲酰胺 在 硝酸 、 溶剂黄146 作用下， 反应 24.0h， 以50%的产率得到2,6-dihydroxy-3-nitrobenzamide
  参考文献：
  名称：

  Bone selective effect of an estradiol conjugate with a novel tetracycline-derived bone-targeting agent

  摘要：

  In this study a novel bone-targeting agent containing elements of the tricarbonylmethane system of ring A of tetracycline was developed and was shown to bind to the mineral constituent of bone, hydroxyapatite. Conjugation of this bone-targeting agent to estradiol resulted in a bone-targeted estrogen (BTE2-A1) with an enhanced ability to bind to hydroxyapatite. In an ovariectomized rat model of osteoporosis a partial separation of the skeletal effects of estradiol from the uterine effects was observed following subcutaneous administration of BTE2-A1. This novel bone-targeting estradiol delivery system has the potential to improve the safety pro. le of estradiol in the treatment of osteoporosis. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.12.051

文献信息

• Compounds for diagnosis, treatment and prevention of bone injury and metabolic disorders
  申请人：Pierce M. William

  公开号：US20050143366A1

  公开（公告）日：2005-06-30

  The present invention relates to compounds of the formula or pharmaceutically acceptable salts thereof useful for the prophylaxis and treatment of degenerative bone disorders and for the acceleration of bone healing.

  本发明涉及以下式的化合物或其药用可接受盐，用于预防和治疗退行性骨疾病以及促进骨愈合。
• Antiparasitic salicylanilide derivatives
  申请人：Janssen Pharmaceutica N.V.

  公开号：US04005218A1

  公开（公告）日：1977-01-25

  Compounds of the class of salicylanilides substituted in the 4-position of the anilino moiety with a --CH(CN)-Ar group wherein Ar is phenyl, substituted phenyl, thienyl, halothienyl or naphthalenyl, said salicylanilides being useful as parasiticides.

  苯甲酰苯胺类化合物，其在苯胺部分的4位上用--CH(CN)-Ar基团进行取代，其中Ar是苯基，取代苯基，噻吩基，卤代噻吩基或萘基，这些苯甲酰苯胺类化合物可用作寄生虫药物。
• Bone selective effect of an estradiol conjugate with a novel tetracycline-derived bone-targeting agent
  作者：Jason R. Neale、Natali B. Richter、Kevyn E. Merten、K. Grant Taylor、Sujan Singh、Leonard C. Waite、Nicole K. Emery、Ned B. Smith、Jian Cai、William M. Pierce

  DOI：10.1016/j.bmcl.2008.12.051

  日期：2009.2

  In this study a novel bone-targeting agent containing elements of the tricarbonylmethane system of ring A of tetracycline was developed and was shown to bind to the mineral constituent of bone, hydroxyapatite. Conjugation of this bone-targeting agent to estradiol resulted in a bone-targeted estrogen (BTE2-A1) with an enhanced ability to bind to hydroxyapatite. In an ovariectomized rat model of osteoporosis a partial separation of the skeletal effects of estradiol from the uterine effects was observed following subcutaneous administration of BTE2-A1. This novel bone-targeting estradiol delivery system has the potential to improve the safety pro. le of estradiol in the treatment of osteoporosis. (c) 2008 Elsevier Ltd. All rights reserved.