N'-dodecanoylisonicotinohydrazide | 6312-52-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: N'-dodecanoylisonicotinohydrazide
• 英文别名: isoniazid-lauric acid；N-isonicotinoyl-N'-lauroyl hydrazine；N-Isonicotinoyl-N'-lauroyl-hydrazin；N-Isonicotinoyl-N'-dodecanoyl-hydrazin；N'-dodecanoylpyridine-4-carbohydrazide
• CAS: 6312-52-3
• 化学式: C₁₈H₂₉N₃O₂
• 分子量: 319.447
• InChiKey: HEKMDVBJCMXAHG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  23
• 可旋转键数：
  11
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  71.1
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  异烟肼 、 月桂酰氯 在 三乙胺 作用下， 以 氯仿 为溶剂， 反应 96.0h， 生成 N'-dodecanoylisonicotinohydrazide
  参考文献：
  名称：

  [EN] YEAST CELL WALL PARTICLE ENCAPSULATION OF BIODEGRADABLE PRO-PAYLOADS
  [FR] ENCAPSULATION DE PARTICULES DE PAROI DE CELLULE DE LEVURE DE PROCHARGES UTILES BIODÉGRADABLES

  摘要：

  本公开提供了一种颗粒传递系统，包括提取的酵母细胞壁，其中包括β-葡聚糖，以及包含荷载支架分子的前荷载分子，通过可切割的连接剂可操作地和可逆地连接到荷载分子。本公开还提供了制备该颗粒传递系统的方法和使用该系统的方法。

  公开号：

  WO2019178443A1

文献信息

• Chemotherapy of Experimental Tuberculosis. VIII. The Synthesis of Acid Hydrazides, their Derivatives and Related Compounds^1,2
  作者：Harry L. Yale、Kathryn Losee、Joseph Martins、Mary Holsing、Frances M. Perry、Jack Bernstein

  DOI：10.1021/ja01104a046

  日期：1953.4
• DE957572
  申请人：——

  公开号：——

  公开（公告）日：——
• A thermo-responsive and self-healing liposome-in-hydrogel system as an antitubercular drug carrier for localized bone tuberculosis therapy
  作者：Peng Liu、Binbin Guo、Shengfeng Wang、Jinsong Ding、Wenhu Zhou

  DOI：10.1016/j.ijpharm.2018.12.083

  日期：2019.3

  Isoniazid (INH) is a first-line therapy for bone tuberculosis (TB), but its clinic benefits are limited by severe side-effects after long-time administration. While nano-drug delivery systems present as promising strategies for INH delivery, the therapeutic efficacies are usually suboptimal due to ineffective drug accumulation at diseased sites. Local delivery system can achieve high drug concentration at focus sites with minimal systemic exposure, and herein we aimed to employ this strategy to develop a novel liposome-in-hydrogel system for localized treatment of bone TB. To achieve sustainable drug release, a derivative of INH called DINH was loaded because of its hydrophobicity, as well as its better activity and higher biosafety than INH. The hybrid system was demonstrated for thermo-responsive and self-healing properties via phase transition test and rheological studies, which were particularly useful for intra-articular administration. In vivo microdialysis studies revealed that the system can rapidly release drug into synovial fluid to reach effective inhibitory concentrations after localized injection, followed by a steady-state drug release. The optical image studies were performed to study its long-term behavior in vivo, which suggested a sustained drug release profile for several days. This work provides a promising drug delivery system for bone TB therapy.
• ISONIAZID MEDIATED HEALING OF WOUNDS AND ULCERS
  申请人：Pharma 2100

  公开号：EP2068873A2

  公开（公告）日：2009-06-17
• [EN] ISONIAZID MEDIATED HEALING OF WOUNDS AND ULCERS<br/>[FR] GUÉRISON DES BLESSURES ET DES ULCÈRES SOUS LA MÉDIATION DE L'ISONIAZIDE
  申请人：PHARMA 2100

  公开号：WO2008031440A2

  公开（公告）日：2008-03-20

  [EN] The invention relates to the use of a compound(s) selected from isoniazid and isoniazid analogs of formula Ia, wherein R is -C(O)NHNH₂, -C(O)NHNHC_1-6 alkyl, -C(O)NHN=C₁-₆ alkenyl, -C(O)NHNHC_2-6 alkenyl, -C(O)NHC_1-6 alkyl, -C(O)NHC_2-6 alkenyl, -C(O)NHNHC(O)C_1-6alkyl, -NHC(O)C_1-6 alkyl, -NHC(O)C_1-6 alkenyl, -NHC(O)NH₂, -NHC(O)NHC_1-6 alkyl, -NHC(O)NHC_2-6 alkenyl, or -COOH, and wherein formula (Ia) optionally is further substituted with one or more substituents; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the preparation of a pharmaceutical composition for treating a condition selected from the group consisting of cutaneous lesions, wounds, ulcers and infarcts in a tissue area with compromised vascularisation, in an animal, such as a human subject. The compound is preferably isoniazid, or pharmaceutical acceptable salts, solvates or prodrugs thereof, and the conditions to be treated is for example selected from the group consisting of pressure ulcers, diabetic ulcers, arterial ulcers and anastomotic ulcers. The invention furthermore relates to a method of treating a condition selected from wounds, ulcers or infarcts in a tissue area with compromised vascularisation in an animal, such as a human subject.
  [FR] La présente invention concerne l'utilisation d'un ou de plusieurs composés choisis parmi l'isoniazide et des analogues de l'isoniazide de formule (Ia), dans laquelle R est -C(O)NHNH₂, -C(O)NHNH-alkyle en C_1-6, -C(O)NHN=alkényle en C₁-₆, -C(O)NHNH-alkényle en C_2-6, -C(O)NH-alkyle en C_1-6, -C(O)NH-alkényle en C_2-6, -C(O)NHNHC(O)-alkyle en C_1-6, -NHC(O)-alkyle en C_1-6, -NHC(O)-alkényle en C_1-6, -NHC(O)NH₂, -NHC(O)NH-alkyle en C_1-6, -NHC(O)NH-alkényle en C_2-6 ou -COOH, la formule (Ia) étant en outre facultativement substituée avec un ou plusieurs substituants ; ou leurs sels, solvates ou promédicaments pharmaceutiquement acceptables, pour la préparation d'une composition pharmaceutique destinée au traitement d'une affection choisie dans le groupe comprenant les lésions cutanées, les blessures, les ulcères et les infarctus dans une zone tissulaire à vascularisation altérée, chez un animal tel qu'un sujet humain. De préférence, le composé est l'isoniazide ou ses sels, solvates ou promédicaments pharmaceutiquement acceptables et l'affection à traiter est choisie par exemple dans le groupe comprenant les ulcères de décubitus, les ulcères diabétiques, les ulcères artériels et les ulcères peptiques. L'invention concerne en outre un procédé de traitement d'une affection choisie parmi les blessures, les ulcères et les infarctus dans une zone tissulaire à vascularisation altérée chez un animal tel qu'un sujet humain.