2-乙基苯肼 | 59635-98-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 2-乙基苯肼
• 英文名称: o-ethylbenzoyl hydrazide
• 英文别名: 2-ethylbenzoic acid hydrazide；2-ethyl benzohydrazide；2-Ethylbenzohydrazide
• CAS: 59635-98-2
• 化学式: C₉H₁₂N₂O
• 分子量: 164.207
• InChiKey: PRGOMJUDGZDSQZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-乙基苯肼 以 乙二醇乙醚 、 二氯甲烷 、 乙腈 为溶剂， 以96,27 mg (72.6%)的产率得到3-(2-乙基苯基)-5-(3-甲氧基苯基)-1H-1,2,4-三唑
  参考文献：
  名称：

  Use of nitrogen heterocyclic aromatic derivatives in the topical treatment of the epithelial tissues diseases

  摘要：

  通用化学式L(I)和(IV)的衍生物被用于局部治疗上皮组织疾病，如银屑病（表皮）和溃疡性结肠炎（下肠）。这些化合物在治疗皮肤病如银屑病、特应性皮炎等类似疾病时，例如通过经皮途径给药时，显示出很高的功效，或者在治疗下肠上皮疾病如溃疡性结肠炎和克罗恩病时，通过口服或直肠途径给药。

  公开号：

  US06323230B1
• 作为产物：
  描述：

  在 盐酸 作用下， 反应 0.5h， 生成 2-乙基苯肼
  参考文献：
  名称：

  A new class of nonhormonal pregnancy-terminating agents. Synthesis and contragestational activity of 3,5-diaryl-s-triazoles

  摘要：

  A series of 3,5-diaryl-s-triazoles were synthesized and evaluated as postimplantation contragestational agents. The introduction of various substituents (e.g., an o-alkyl chain on one phenyl and a m-alkoxy group on the other) was found to increase the potency. Several compounds with very high pregnancy-terminating activity in both hamsters and rats were obtained. One of these, 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-s-triazole, DL 111 (36), was selected for detailed evaluation in various animal species. A synthetic scheme for the preparation of these compounds and preliminary structure-activity relationships are presented.

  DOI：

  10.1021/jm00362a018

文献信息

• THIAZEPINE DERIVATIVE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2119719A1

  公开（公告）日：2009-11-18

  The present invention relates to a thiazepine derivative or a pharmacologically acceptable salt thereof having an excellent effect of inhibiting 11β-hydroxysteroid dehydrogenase type 1. A thiazepine derivative or a pharmacologically acceptable salt thereof having general formula (I): wherein R1 represents a hydrogen atom, a C1-C6 alkyl group or the like; R2 represents a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C1-C6 hydroxyalkyl group, or the like; R3 represents a hydrogen atom or a C1-C6 alkyl group; R4 represents a C6-C10 aryl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group a or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group a; Substituent Group a consists of a halogen atom, a C1-C6 alkyl group, a C6-C10 aryl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group b, and so forth; Substituent Group b consists of a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, and so forth.

  本发明涉及一种噻吩啶衍生物或其药理学上可接受的盐，具有优异的抑制11β-羟基类固醇脱氢酶1型的作用。具有通式（I）的噻吩啶衍生物或其药理学上可接受的盐： 其中 R1代表氢原子、C1-C6烷基或类似物；R2代表C1-C6烷基、C1-C6卤代烷基、C1-C6羟基烷基或类似物；R3代表氢原子或C1-C6烷基；R4代表可能被1至5个独立选择自取代基团a的基团取代的C6-C10芳基，或可能被1至3个独立选择自取代基团a的基团取代的杂环基团；取代基团a由卤原子、C1-C6烷基、可能被1至5个独立选择自取代基团b的基团取代的C6-C10芳基等组成；取代基团b由卤原子、C1-C6烷基、C1-C6卤代烷基等组成。
• ＺＮＦ１４３阻害活性を有する化合物およびその利用
  申请人：株式会社ヤクルト本社

  公开号：JP2016124812A

  公开（公告）日：2016-07-11

  【課題】ZNF143阻害効果を有する化合物並びにこれを含むZNF143阻害剤及び医薬組成物の提供。【解決手段】式（Ｉ）で表される化合物又はその塩並びにそれを含むZNF143阻害剤及びそれを有効成分とする医薬組成物。Ａ−Ｂ−Ｃ−Ｄ（Ｉ）［ＡはＨ、メチル基、ナフチル基、フェニル基又は含窒素複素環；Ｂは、であり、Ｃは、アミド結合又はＮとＯを含有する複素芳香環；Ｄは置換／未置換のフェニル基又は単環のＮ或いはＳを含む複素芳香環；Ｃ及びＤは共に、置換基を有していてもよい縮合複素環等］【選択図】図１

  提供具有ZNF143抑制作用的化合物以及包含该化合物的ZNF143抑制剂和药物组合物。通过式（I）表示的化合物或其盐，以及包含它的ZNF143抑制剂和以其为有效成分的药物组合物。A-B-C-D（I）[其中A为氢、甲基、萘基、苯基或含氮杂环；B为，C为，含有酰胺键或含氮和氧的复杂芳香环；D为取代/未取代的苯基或含有单环的N或S的复杂芳香环；C和D均可具有取代基，也可以是融合的复杂环等]【选图】图1
• OREXIN RECEPTOR ANTAGONISTS WHICH ARE [ORTHO BI-(HETERO-)ARYL]-[2-(META BI-(HETERO-)ARYL)-PYRROLIDIN-1-YL]-METHANONE DERIVATIVES
  申请人：ACTELION PHARMACEUTICALS LTD

  公开号：US20150252032A1

  公开（公告）日：2015-09-10

  The present invention relates to [ortho bi-(hetero-)aryl]-[2-(meta bi-(hetero-)aryl)-pyrrolidin-1-yl]-methanone derivatives of formula (I) wherein R, and the rings A 1 A 2 and A 3 are as described in the description, to pharmaceutically acceptable salts thereof, to their preparation, to pharmaceutical compositions containing one or more compounds of formula (I), and to their use as pharmaceuticals, especially to their use as orexin receptor antagonists.

  本发明涉及公式（I）的[ortho bi-（hetero-）aryl]-[2-（meta bi-（hetero-）aryl）-pyrrolidin-1-yl]-methanone衍生物，其中R和环A1A2和A3如描述中所述，以及其药学上可接受的盐、其制备方法、含有一个或多个公式（I）化合物的制药组合物以及它们作为药物的用途，特别是作为促进睡眠激素受体拮抗剂的用途。
• Synthesis of 2-aryl-5-(arylsulfonyl)-1,3,4-oxadiazoles as potent antibacterial andantioxidant agents
  作者：S N MURTHY BODDAPATI、SUBRAHMANYAM TALARI、A EMMANUEL KOLA、BHUVANESWARI CHALAPAKA

  DOI：10.55730/1300-0527.3366

  日期：——

  Ten novel 2-aryl-5-(arylsulfonyl)-1,3,4-oxadiazoles were produced and assessed for their in vitro antibacterial and antioxidant activities. Diverse spectroscopic methods li1H NMR, 13C NMR, IR, and LCMS were used for the characterization of the prepared samples and all the data was in good agreement with the anticipated structures. The prepared compounds 6a-j were screened for their in vitro antibacterial activity against bacterial strains Pseudomonas aeruginosa, Enterobacter aerogenes, Escherichia coli (grampositive), and Bacillus cerus, Staphylococcus aureus, Bacillus subtilis (gram-negative). The antimicrobial screening outcome revealed that the prepared 2-(3,4-dimethylphenyl)-5-tosyl-1,3,4-oxadiazole (6j), 2-(3-isopropylphenyl)-5-tosyl-1,3,4-oxadiazole (6c), and 2-(2-ethylphenyl)-5-tosyl-1,3,4-oxadiazole (6i) are most potent among all the examined compounds. Furthermore, the antioxidant activity of the prepared compounds was also investigated by DPPH radical scavenging method and the results showed that some of the compounds were moderately active.

  制备了十种新型2-芳基-5-(芳基磺酰基)-1,3,4-恶二唑，并评估了它们的体外抗菌和抗氧化活性。采用多种光谱方法（li1H NMR、13C NMR、IR和LCMS）对制备的样品进行了表征，所有数据与预期的结构一致。对制备的化合物6a-j进行了体外抗菌活性筛选，以对抗铜绿假单胞菌、产气肠杆菌、大肠杆菌（革兰氏阳性）和蜡样芽孢杆菌、金黄色葡萄球菌、枯草芽孢杆菌（革兰氏阴性）等菌株。抗菌筛选结果表明，在所研究的化合物中，制备的2-(3,4-二甲基苯基)-5-对甲苯磺酰基-1,3,4-恶二唑（6j）、2-(3-异丙基苯基)-5-对甲苯磺酰基-1,3,4-恶二唑（6c）和2-(2-乙基苯基)-5-对甲苯磺酰基-1,3,4-恶二唑（6i）的抗菌活性最强。此外，还采用DPPH自由基清除法研究了制备的化合物的抗氧化活性，结果表明，其中一些化合物具有中等活性。
• Neelima; Bhaduri, A. P., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1983, vol. 22, # 1, p. 79 - 80
  作者：Neelima、Bhaduri, A. P.

  DOI：——

  日期：——