Achromycin | 890407-48-4

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 四环素类
• 英文名称: Achromycin
• 英文别名: tetracycline
• CAS: 890407-48-4
• 化学式: C₂₂H₂₄N₂O₈
• 分子量: 444.441
• InChiKey: OFVLGDICTFRJMM-MXAWKICOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.21
• 重原子数：
  32.0
• 可旋转键数：
  2.0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  181.62
• 氢给体数：
  6.0
• 氢受体数：
  9.0

反应信息

• 作为反应物：
  描述：

  copper(II) perchlorate hexahydrate 、 Achromycin 、 邻菲罗啉 以 甲醇 、 水 为溶剂， 以61%的产率得到[Cu(tetracycline)(1,10-phenanthroline)(water)(perchlorate)](ClO4)
  参考文献：
  名称：

  铜（II）与四环素或强力霉素和1,10-邻菲咯啉的两种新三元络合物及其抗肿瘤潜力：细胞毒性和DNA裂解

  摘要：

  本文报道了两种新型三元铜（II）配合物的合成和表征：[Cu（强力霉素）（1,10-菲咯啉）（H 2 O）（ClO 4）]（ClO 4）（1）和[Cu （四环素）（1,10-菲咯啉）（H 2 O）（ClO 4）]（ClO 4）（2）。这些化合物在铜周围表现出扭曲的四边形几何形状，并与两个双齿配体，1,10-菲咯啉和四环素或强力茶碱，一个水分子以及一个在轴向位置上弱结合的高氯酸根离子配位。在这两种化合物中，铜（II）均通过环A上的羟基氧和酰胺基上的氧与四环素结合，并通过其两个杂环氮与1,10-菲咯啉结合。我们已经评估了新复合物与DNA的结合，它们的裂解能力，细胞毒性活性以及在肿瘤细胞中的摄取。复合物优先通过大沟与DNA结合，然后通过涉及ROS生成的氧化机制切割其链。自由基抑制剂和/或捕集剂（例如超氧化物歧化酶，DMSO，和铜（I）螯合剂浴铜。T4 DNA连接酶不能释放DNA裂解产物，这表明该裂

  DOI：

  10.1021/ic101791r
• 作为产物：
  描述：

  6-deoxy-6-hydroperoxy-5a,11a-dehydrotetracycline 在 palladium on activated charcoal 氢气 作用下， 以 甲醇 为溶剂， 反应 2.5h， 以49%的产率得到Achromycin
  参考文献：
  名称：

  The total synthesis of tetracycline

  摘要：

  DOI：

  10.1021/ja00274a072

文献信息

• Synthesis of tetracyclines and analogues thereof
  申请人：President and Fellows of Harvard College

  公开号：US11192866B2

  公开（公告）日：2021-12-07

  The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

  过去 50 年来，四环素类抗生素在治疗传染病方面发挥了重要作用。然而，随着四环素类药物在人类和兽医领域使用的增加，许多以前对四环素类抗生素易感的生物产生了抗药性。所述四环素和四环素类似物的模块化合成提供了一种高效的对映选择性途径，可获得以前通过早期的四环素合成和半合成方法无法获得的各种四环素类似物和多环化合物。这些类似物可用作治疗人类或其他动物疾病的抗微生物剂或抗增殖剂。
• Combinations comprising dibromopropamidine or diminazene and a tetracycline anti-bacterial agent
  申请人：UNION therapeutics A/S

  公开号：US11213533B2

  公开（公告）日：2022-01-04

  This invention relates to combination products comprising an amidine selected from dibromopropamidine and diminazene or a pharmaceutically acceptable salt or solvate thereof; and a tetracycline anti-bacterial agent. The combination products are suitable for use in the treatment of bacterial infections or diseases.

  本发明涉及由选自二溴丙脒和地米那嗪的脒或其药学上可接受的盐或溶液，以及四环素类抗菌剂组成的组合产品。该组合产品适用于治疗细菌感染或疾病。
• Co-administration of dehydroepiandrosterone (DHEA) congener with pharmaceutically active agents for treating inflammation
  申请人：Patel Dinesh

  公开号：US20060004076A1

  公开（公告）日：2006-01-05

  The present invention is related to therapeutic uses of dehydroepiandrosterone (DHEA) congeners. More specifically, the present invention relates to the co-administration of a dehydroepiandrosterone (DHEA) congener in combination with at least one other pharmaceutically active agent to reduce inflammation.
• Delivery System for Functional Compounds
  申请人：Lye Jason

  公开号：US20100215754A1

  公开（公告）日：2010-08-26

  A delivery system for various functional compounds is disclosed. The delivery system incorporates a composition containing alumina. Various functional materials containing particular moieties may be adsorbed onto the alumina and used as desired. The functional compounds can be, for instance, pharmaceuticals, xenobiotics, anti-microbial agents, anti-viral agents, UV absorbers, odor control agents, fragrances, and the like. In one particular embodiment, for instance, certain dyes can be adsorbed onto the alumina surfaces. Once the dye is adsorbed onto the alumina surface, the resulting particles can be combined with a liquid vehicle for use in any suitable printing process.
• COMBINATIONS COMPRISING DIBROMOPROPAMIDINE OR DIMINAZENE AND A TETRACYCLINE ANTI-BACTERIAL AGENT
  申请人：UNION therapeutics A/S

  公开号：US20190201422A1

  公开（公告）日：2019-07-04

  This invention relates to combination products comprising an amidine selected from dibromopropamidine and diminazene or a pharmaceutically acceptable salt or solvate thereof; and a tetracycline anti-bacterial agent. The combination products are suitable for use in the treatment of bacterial infections or diseases.