芬乙嗪 | 522-24-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 中文名称: 芬乙嗪
• 中文别名: 胺乙吩嗪
• 英文名称: fenethazine
• 英文别名: N,N-dimethyl-2-(10H-phenothiazin-10-yl)ethan-1-amine；Fenethazin；dietazina；Phenethazin；N,N-dimethyl-2-phenothiazin-10-ylethanamine
• CAS: 522-24-7
• 化学式: C₁₆H₁₈N₂S
• 分子量: 270.398
• InChiKey: PFAXACNYGZVKMX-UHFFFAOYSA-N

物化性质

• 沸点：
  bp1 183-187°

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  31.8
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2934300000

反应信息

• 作为反应物：
  描述：

  芬乙嗪 在 三乙胺 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 3.0h， 生成 N-methyl-2-phenothiazin-10-yl-ethanamine
  参考文献：
  名称：

  NB 06: From a simple lysosomotropic aSMase inhibitor to tools for elucidating the role of lysosomes in signaling apoptosis and LPS-induced inflammation

  摘要：

  Ceramide generation is involved in signal transduction of cellular stress response, in particular during stress-induced apoptosis in response to stimuli such as minimally modified Low-density lipoproteins, TNFalpha and exogenous C-6-ceramide. In this paper we describe 48 diverse synthetic products and evaluate their lysosomotropic and acid sphingomyelinase inhibiting activities in macrophages. A stimuli induced increase of C-16-ceramide in macrophages can be almost completely suppressed by representative compound NB 06 providing an effective protection of macrophages against apoptosis. Compounds like NB 06 thus offer highly interesting fields of application besides prevention of apoptosis of macrophages in atherosclerotic plaques in vessel walls. Most importantly, they can be used for blocking pH dependent lysosomal processes and enzymes in general as well as for analyzing lysosomal dependent cellular signaling. Modulation of gene expression of several prominent inflammatory messengers IL1B, IL6, IL23A, CCL4 and CCL20 further indicate potentially beneficial effects in the field of (systemic) infections involving bacterial endotoxins like LPS or infections with influenza A virus. (C) 2017 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2017.09.021
• 作为产物：
  描述：

  吩噻嗪-10-碳酰氯 以 苯 为溶剂， 反应 12.5h， 生成 芬乙嗪
  参考文献：
  名称：

  Synthetic applications and mechanism of the pyrolysis of phenothiazine carbamates

  摘要：

  DOI：

  10.1021/jo01292a048

文献信息

• Oral pharmaceutical compositions containing cyclodextrins as taste masking agent
  申请人：——

  公开号：US20040115258A1

  公开（公告）日：2004-06-17

  The application discloses oral pharmaceutical compositions which are tasted in the mouth during administration. Fast-dissolving tablets, chewable tablets and effervescent dispersions are exemplified. To mask the taste of unpleasant-tasting active ingredients, it has been found that blending with cyclodextrin without the conventional complex formation is effective. Consequently more economical modes of manufacture such as simple granulation and dry blending can be used.

  该申请揭示了口服制剂，其在给药过程中在口腔中被品尝。快速溶解片剂、可咀嚼片剂和泡腾分散剂是示例。为了掩盖令人不愉快的活性成分的味道，发现与β-环糊精混合而无需传统的复合形成是有效的。因此，可以使用更经济的制造方式，如简单的制粒和干混合。
• COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES
  申请人：Johansen Lisa M.

  公开号：US20100009970A1

  公开（公告）日：2010-01-14

  The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

  本发明涉及用于治疗病毒性疾病的组合物、方法和试剂盒。在某些实施方式中，病毒性疾病是由单链RNA病毒、黄病毒科病毒或肝病毒引起的。在特定实施方式中，病毒性疾病是病毒性肝炎（例如甲型肝炎、乙型肝炎、丙型肝炎、丁型肝炎、戊型肝炎），药剂或药剂组合包括舍曲林、舍曲林类似物、UK-416244或UK-416244类似物。还包括用于鉴定可用于治疗病毒性疾病的新化合物的筛选方法。
• A convenient procedure for the synthesis of phenothiazine drugs.
  作者：HERVE GALONS、MARCEL MIOCQUE、CLAUDE COMBET-FARNOUX、YOUNES BENSAID、GUY DECODTS、GEORGES BRAM

  DOI：10.1248/cpb.33.5108

  日期：——

  Alkylation of phenothiazines to prepare chlorpromazine and analogous compounds was achieved by solid-liquid phase-transfer catalysis in the presence of Aliquat 336 in the absence of any organic solvent. This simple procedure is easy and rapid.

  在不使用任何有机溶剂的情况下，通过固液相转移催化法实现了吩噻嗪的烷基化，从而制备出氯丙嗪和类似化合物。这种简单的程序既方便又快捷。
• [EN] NEW CLASS OF ANTIBIOTICS HAVING LOW MIC-VALUES TOWARDS DIFFERENT STRAINS OF BACTERIA<br/>[FR] NOUVELLE CLASSE D'ANTIBIOTIQUES AYANT DE FAIBLES CONCENTRATIONS MINIMALES INHIBITRICES (CMI) À L'ÉGARD DE DIFFÉRENTES SOUCHES DE BACTÉRIES
  申请人：UNIV COPENHAGEN

  公开号：WO2020216777A1

  公开（公告）日：2020-10-29

  The present invention relates to a composition comprising a compound of formula (I) wherein X is selected from the group consisting of S, Se, P, PO, SO, NR1, CR1, CR1R1 or C0-2-alkyl; Z is selected from the group consisting of hydrogen, a halogen, SR4, OR4, COR4 where R4 is a C1-12-alkyl; each R2 is independently selected from the group consisting of C1-6-alkyl, halogen, C3-8-cycloalkyl, OH, NH2, NHR1, N(R1)2, O-C1-6-alkyl, O-C3-8-cycloalkyl, NH-C1-6-alkyl, NH-C3-8- cycloalkyl, S-C1-6-alkyl, S-C3-8-cycloalkyl, aryl, heteroaryl, aryloxy, heteroaryloxy, arylamino, heteroarylamino, arylalkyl, heteroarylalkyl, arylalkyloxy and heteroarylalkyloxy; d is selected from 0, 1, 2, and 3; each R3 is independently selected from the group consisting of C1-6-alkyl, halogen, C3-8-cycloalkyl, OH, NH2, NHR1, N(R1)2, O-C1-6-alkyl, O-C3-8-cycloalkyl, NH-C1-6-alkyl, NH-C3-8-cycloalkyl, S-C1-6-alkyl, S-C3-8-cycloalkyl, aryl, heteroaryl, aryloxy, heteroaryloxy, arylamino, heteroarylamino, arylalkyl, heteroarylalkyl, arylalkyloxy and heteroarylalkyloxy; e is selected from 0, 1, 2, 3, and 4; R1 is selected from the group consisting of C1-6-alkyl, C3-8-cycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl; R5 is N-(CHW)-N(Y1)(Y2)(Y3) or C=CH-(CHW)-N(Y1)(Y2)(Y3); each W is individually selected from the group consisting of linear or branched C1-6-alkyl or together with the nitrogen atom - N(Y1)(Y2)(Y3) - to which it is attached forms an optionally substituted nitrogen-containing heteroaryl or optionally substituted nitrogen-containing heterocyclyl together with Y1 where; Y1 is selected from the group consisting of C1-12-alkyl or together with the W and the nitrogen atom to which it is attached forms an optionally substituted nitrogen-containing heteroaryl or optionally substituted nitrogen-containing heterocyclyl; Y2 is selected from the group consisting of C1-12-alkyl; Y3 is selected from the group consisting of linear or branched C2-25-alkyl, linear or branched C2-25 alkenyl or linear or branched C2-25 alkynyl; where A is selected from any pharmaceutical relevant/acceptable anion/counterion; wherein if X is S and Z is a halogen then Y3 cannot be a C2-alkyl or a branched C3-alkyl; wherein if X is S and Z is hydrogen then Y3 cannot be C2-alkyl or linear or branched C5-alkyl. The invention also relates to anti-microbial composition for use as a medicament and for use in treating a microbial infection in a human subject.

  本发明涉及一种组合物，该组合物包括以下式(I)的化合物，其中X从S、Se、P、PO、SO、NR1、CR1、CR1R1或C0-2-烷基组成的群中选择；Z从氢、卤素、SR4、OR4、COR4选择，其中R4是C1-12-烷基；每个R2独立地从C1-6-烷基、卤素、C3-8-环烷基、OH、NH2、NHR1、N(R1)2、O-C1-6-烷基、O-C3-8-环烷基、NH-C1-6-烷基、NH-C3-8-环烷基、S-C1-6-烷基、S-C3-8-环烷基、芳基、杂环芳基、芳氧基、杂芳氧基、芳基氨基、杂芳基氨基、芳基烷基、杂芳基烷基、芳基氧基和杂芳基氧基组成的群中选择；d从0、1、2和3中选择；每个R3独立地从C1-6-烷基、卤素、C3-8-环烷基、OH、NH2、NHR1、N(R1)2、O-C1-6-烷基、O-C3-8-环烷基、NH-C1-6-烷基、NH-C3-8-环烷基、S-C1-6-烷基、S-C3-8-环烷基、芳基、杂环芳基、芳氧基、杂芳氧基、芳基氨基、杂芳基氨基、芳基烷基、杂芳基烷基、芳基氧基和杂芳基氧基组成的群中选择；e从0、1、2、3和4中选择；R1从C1-6-烷基、C3-8-环烷基、芳基、杂环芳基、芳基烷基、杂芳基烷基组成的群中选择；R5是N-(CHW)-N(Y1)(Y2)(Y3)或C=CH-(CHW)-N(Y1)(Y2)(Y3)；每个W单独从线性或支链的C1-6-烷基组成的群中选择，或者与氮原子-N(Y1)(Y2)(Y3)-形成一个可选择取代的含氮杂芳基或可选择取代的含氮杂环烷基，其中；Y1从C1-12-烷基中选择，或者与W和连接的氮原子形成一个可选择取代的含氮杂芳基或可选择取代的含氮杂环烷基；Y2从C1-12-烷基中选择；Y3从线性或支链的C2-25-烷基、线性或支链的C2-25-烯烃基或线性或支链的C2-25-炔烃基中选择；其中A从任何药用相关/可接受的阴离子/对离子中选择；其中如果X是S且Z是卤素，则Y3不能是C2-烷基或支链C3-烷基；其中如果X是S且Z是氢，则Y3不能是C2-烷基或线性或支链的C5-烷基。该发明还涉及用作药物和用于治疗人体主体中的微生物感染的抗微生物组合物。
• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。