2-methyl-2-phenyl propanoyl hydrazide | 5809-15-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-methyl-2-phenyl propanoyl hydrazide
• 英文别名: 2-methyl-2-phenylpropione hydrazide；2-methyl-2-phenylpropanehydrazide
• CAS: 5809-15-4
• 化学式: C₁₀H₁₄N₂O
• mdl: MFCD09802904
• 分子量: 178.234
• InChiKey: MQXCWWHSWXLWPJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 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-methyl-2-phenyl propanoyl hydrazide 在 溶剂黄146 、 三氯氧磷 作用下， 以 乙醇 为溶剂， 反应 5.02h， 生成 1-(2-methyl-2-phenylpropanoyl)-3-phenylpyrazole-4-carbaldehyde
  参考文献：
  名称：

  Kidwai; Aryal; Misra, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2001, vol. 40, # 8, p. 717 - 718

  摘要：

  DOI：
• 作为产物：
  描述：

  2-甲基-2-苯基丙酸乙酯 在 一水合肼 作用下， 生成 2-methyl-2-phenyl propanoyl hydrazide
  参考文献：
  名称：

  Kidwai; Aryal; Misra, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2001, vol. 40, # 8, p. 717 - 718

  摘要：

  DOI：

文献信息

• Synthesis, spectral characterization and biological evaluation of a novel series of 6-arylsubstituted-3-[2-(4-substitutedphenyl)propan-2-yl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines
  作者：Pushpan Puthiyapurayil、Boja Poojary、Chandrashekhar Chikkanna、Sunil Kumar Buridipad

  DOI：10.1016/j.ejmech.2012.06.059

  日期：2012.11

  On account of the reported anticancer activity of triazolothiadiazines, we have synthesized a novel series of 6-arylsubstituted-3-[2-(4-substitutedphenyl)propan-2-yl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and tested for in-vitro cytotoxicity by trypan blue exclusion and MTT assay. These compounds were also evaluated for their in-vivo anthelmintic activity, as well as in-vitro antimicrobial studies

  由于已报道的三唑并噻二嗪具有抗癌活性，我们合成了一系列新的6-芳基取代的-3- [2-（4-取代的苯基）丙烷-2-基] -7H- [1,2,4]三唑[3] ，4- b ] [1,3,4]噻二嗪，并通过台盼蓝排除法和MTT法测试了体外细胞毒性。还评估了这些化合物的体内驱虫活性以及体外抗菌研究。在测试的化合物中，化合物7j是最有希望的细胞毒性剂，在MCF-7细胞中的IC 50值为10.54μM。化合物7l和7q表现出优异的驱虫活性。化合物7d，7f，7j，7l，7o，7p和7r显示出良好的抗菌活性，而化合物7e和7k显示出优异的抗真菌活性。通过IR，1 H NMR，13 C NMR和LCMS分析表征新合成的化合物的结构。
• Alkyl substituted triazole compounds as agonists of the APJ Receptor
  申请人：AMGEN INC.

  公开号：US11191762B2

  公开（公告）日：2021-12-07

  Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I), (II) where the definitions of the variables are provided herein.

  式 I 和式 II 的化合物、其药学上可接受的盐、前述任何化合物的立体异构体或其混合物是 APJ 受体的激动剂，可用于治疗心血管疾病和其他疾病。式 I 和式 II 的化合物具有如下结构：(I)、(II) 变量的定义见本文。
• Biarylpyrazolyl Oxadiazole as Potent, Selective, Orally Bioavailable Cannabinoid-1 Receptor Antagonists for the Treatment of Obesity
  作者：Suk Ho Lee、Hee Jeong Seo、Sung-Han Lee、Myung Eun Jung、Ji-Hyun Park、Hyun-Ju Park、Jakyung Yoo、Hoseop Yun、Jooran Na、Suk Youn Kang、Kwang-Seop Song、Min-ah Kim、Chong-Hwan Chang、Jeongmin Kim、Jinhwa Lee

  DOI：10.1021/jm800843r

  日期：2008.11.27

  Since the CB1 cannabinoid receptor antagonist 1 (SR141716, rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In the present study, biarylpyrazole analogues based on a pyrazole core coupled with 1,3,4-oxadiazole were synthesized and tested for CB1 receptor binding affinity. Thorough SAR studies to optimize pyrazole substituents as well as 1,3,4-oxadiazole ring led to several novel CB1 antagonists with IC50 similar to 1 nM for the CB1 receptor binding. Among these analogues, we identified 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-pyrazol-3-yl)-5-(1-(trifluoromethyl)cyclopropyl)-1,3,4-oxa- diazole 43c as a promising precandidate for the development as an antiobesity agent.
• Structure–activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors
  作者：Lijie Peng、Lei Duan、Xiaofeng Liu、Mengjie Shen、Yingjun Li、Jiajie Yan、Honglin Li、Ke Ding

  DOI：10.1016/j.bmcl.2011.06.009

  日期：2011.8

  A series of alpha-glutamic acid scaffold based 4-(benzamido)-4-(1,3,4-oxadiazol-2-yl) butanoic acids were designed and synthesized as new ADAMTS inhibitors. The compounds dose-dependently inhibited the enzymatic activities of ADAMTS-4 and ADAMTS-5. One of the most active compound 2h potently inhibited ADAMTS-4 and ADAMTS-5 with IC(50) values of 1.2 and 0.8 mu M, respectively. These inhibitors may serve as new lead compounds for further development of therapeutics to treat osteoarthritis. (C) 2011 Elsevier Ltd. All rights reserved.
• Development of Orally Active Nonpeptidic Inhibitors of Human Neutrophil Elastase
  作者：Kazuyuki Ohmoto、Tetsuya Yamamoto、Motohiro Okuma、Toshihide Horiuchi、Hirotoshi Imanishi、Yoshihiko Odagaki、Kazuhito Kawabata、Tomohiko Sekioka、Yasushi Hirota、Shozo Matsuoka、Hisao Nakai、Masaaki Toda、John C. Cheronis、Lyle W. Spruce、Albert Gyorkos、Maciej Wieczorek

  DOI：10.1021/jm000410y

  日期：2001.4.1

  5-Amino-2-phenylpyrimidin-6-ones, some of their desamino derivatives, and miscellaneous derivatives were synthesized and biologically evaluated on both in vitro activity and oral activity in an acute hemorrhagic assay. These compounds contained an alpha -keto-1,3,4-oxadiazole moiety to bind covalently to the Ser-195 hydroxy group of human neutrophil elastase (HNE). Among those tested, compounds 11a-c,e,i-1(F), 11d,e,k(H), ald,e,k(F), and ald,e(H) showed a good oral profile. RS-Mixture 3(H) was selected for clinical evaluation based on its oral potency, duration of action, enzyme selectivity, safety profile, and ease of synthesis. Structure-activity relationships (SARs) are discussed.