histidine hydrazide

• 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: histidine hydrazide
• 英文别名: 2-amino-3-(1H-imidazol-5-yl)propanehydrazide
• 化学式: C₆H₁₁N₅O
• 分子量: 169.186
• InChiKey: HIQSHBQGIXVMBC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.9
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  110
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  histidine hydrazide 、 异氰酸丙基三乙氧基硅烷 以 四氢呋喃 为溶剂， 反应 2.0h， 以89%的产率得到
  参考文献：
  名称：

  Construction of pH responsive periodic mesoporous organosilica with histidine framework (His-PMO) for drug delivery

  摘要：

  pH-responsive drug delivery material based on histidine periodic mesoporous organosilica (His-PMO) was constructed by the condensation of histidine bissilylated organosilica precursor (His-BOP) and TEOS in acidic medium under the template P123. The organosilica precursor His-BOP was prepared by selecting histidine as the main reactant via multi-step reactions. Histidine is first introduced as the skeletal constituents of PMO to improve flexibility of the robust framework and sensitivity of pH response. The materials His-PMO maintain ordered mesostructure and facilitate entrance or exit of compounds during application process. Paclitaxel (PTX) is used as the cargo molecules to observe drug delivery in vitro. The results indicate that the maximum loading amounts of drugs are up to 28 mg/g on the material His-PMO-10% under the same conditions. In the release experiments, the different release percentage and speed of PTX are observed with the variation of pH values (pH 5.2, 6.8 and 7.4), which exhibits nonlinear over the time. Rapid accumulation of drugs at low pH are maybe helpful for improving the performance of conquering cancer.

  DOI：

  10.1016/j.jssc.2019.07.049
• 作为产物：
  描述：

  D,L-histidine 在 氯化亚砜 、 一水合肼 作用下， 以 乙醇 为溶剂， 生成 histidine hydrazide
  参考文献：
  名称：

  Construction of pH responsive periodic mesoporous organosilica with histidine framework (His-PMO) for drug delivery

  摘要：

  pH-responsive drug delivery material based on histidine periodic mesoporous organosilica (His-PMO) was constructed by the condensation of histidine bissilylated organosilica precursor (His-BOP) and TEOS in acidic medium under the template P123. The organosilica precursor His-BOP was prepared by selecting histidine as the main reactant via multi-step reactions. Histidine is first introduced as the skeletal constituents of PMO to improve flexibility of the robust framework and sensitivity of pH response. The materials His-PMO maintain ordered mesostructure and facilitate entrance or exit of compounds during application process. Paclitaxel (PTX) is used as the cargo molecules to observe drug delivery in vitro. The results indicate that the maximum loading amounts of drugs are up to 28 mg/g on the material His-PMO-10% under the same conditions. In the release experiments, the different release percentage and speed of PTX are observed with the variation of pH values (pH 5.2, 6.8 and 7.4), which exhibits nonlinear over the time. Rapid accumulation of drugs at low pH are maybe helpful for improving the performance of conquering cancer.

  DOI：

  10.1016/j.jssc.2019.07.049
• 作为试剂：
  描述：

  curcumin 在 histidine hydrazide 、 对甲苯磺酸 、 溶剂黄146 作用下， 以 乙醇 、 正丁醇 为溶剂， 反应 24.0h， 以22%的产率得到hydrazinocurcumin
  参考文献：
  名称：

  Antitumor Agents. Part 214:††For paper 213, see ref 1. Synthesis and Evaluation of Curcumin Analogues as Cytotoxic Agents

  摘要：

  Fifty-eight curcumin analogues were prepared and evaluated for in vitro cytotoxicity against a panel of human tumor cell lines. Compound 50 was the most potent analogue against several cell lines, including HOS (bone cancer) and 1A9 (breast cancer), with ED50 values of 0.97 and <0.63 mug/mL, respectively. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(02)00249-3

文献信息

• Novel curcumin analogues and uses thereof
  申请人：——

  公开号：US20030203933A1

  公开（公告）日：2003-10-30

  The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

  本发明涉及一种能够作为雄激素受体拮抗剂的化合物、包含该化合物的药物配方以及使用它们的方法。这些用途包括但不限于作为抗肿瘤剂，特别是用于治疗结肠癌、皮肤癌和前列腺癌等癌症，并在患有与雄激素相关的疾病的受试者中诱导雄激素受体拮抗剂活性。雄激素相关疾病的例子包括但不限于脱发、多毛症、行为障碍、痤疮和无抑制的精子生成，其中需要抑制精子生成。
• NOVEL CURCUMIN ANALOGUES AND USES THEREOF
  申请人：Lee Kuo-Hsiung

  公开号：US20080161391A1

  公开（公告）日：2008-07-03

  The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

  本发明涉及能够作为雄激素受体拮抗剂的化合物、含有该化合物的制药配方以及其使用方法。这些用途包括但不限于作为抗肿瘤剂，特别是用于治疗结肠癌、皮肤癌和前列腺癌等癌症，以及在患有雄激素相关疾病的人体内诱导雄激素受体拮抗活性。雄激素相关疾病的例子包括但不限于脱发、多毛症、行为障碍、痤疮以及需要抑制精子生成的不受抑制的精子生成。
• 4-Substituted-2-azetidinone compound, process of producing the compounds, and medicaments containing the compounds
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP0123444A1

  公开（公告）日：1984-10-31

  4-substituted-2-azetidinone compounds shown by the general formula and salts thereof. The compounds of this invention have a strong CNS activity and are useful fortreating disturbance of consciousness in schizophrenia and head injury, hypobulia and memory loss. The compounds may be made by reacting an acid or or a reactive derivative thereof with the appropriate amine or a reactive derivative thereof.

  4-取代的-2-氮杂环丁酮化合物及其盐类。 本发明的化合物具有很强的中枢神经系统活性，可用于治疗精神分裂症和头部损伤中的意识障碍、小脑功能减退和记忆力减退。 这些化合物可通过酸或其活性衍生物与适当的胺或其活性衍生物反应制得。
• Renin-inhibitory oligopeptides, their preparation and use
  申请人：SANKYO COMPANY LIMITED

  公开号：EP0228192A2

  公开（公告）日：1987-07-08

  Oligopeptides of formula (I): where R1R7 are various organic groups and n and m are 0 or 1, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.

  式(I)的寡肽： 其中 R1R7 为各种有机基团，n 和 m 为 0 或 1，具有肾素抑制活性，特别适合口服。它们可以通过传统的肽合成反应缩合其氨基酸组分或低级寡肽来制备。
• EP1494993A4
  申请人：——

  公开号：EP1494993A4

  公开（公告）日：2005-09-14