2-hydroxy-N-(4-(trifluoromethyl)benzoyl)benzamide | 710945-58-7

• 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-hydroxy-N-(4-(trifluoromethyl)benzoyl)benzamide
• 英文别名: MP-IV-20；2-hydroxy-N-[4-(trifluoromethyl)benzoyl]benzamide
• CAS: 710945-58-7
• 化学式: C₁₅H₁₀F₃NO₃
• 分子量: 309.245
• InChiKey: UHQHSGCKGVRYHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-hydroxy-N-(4-(trifluoromethyl)benzoyl)benzamide 在 硫酸 、 sodium methylate 作用下， 以 甲醇 、 乙腈 为溶剂， 反应 7.0h， 生成 2-[4-(2-Hydroxyphenyl)-6-[4-(trifluoromethyl)phenyl]-1,3,5-triazin-2-yl]phenol
  参考文献：
  名称：

  NEW TRIAZINE DERIVATIVE, ULTRAVIOLET ABSORBER, AND RESIN COMPOSITION

  摘要：

  公开号：

  EP2460799B1
• 作为产物：
  描述：

  4-三氟甲基苯甲酰氯 、 水杨酰胺 在 吡啶 作用下， 反应 4.0h， 以29%的产率得到2-hydroxy-N-(4-(trifluoromethyl)benzoyl)benzamide
  参考文献：
  名称：

  Synthesis, Biological Evaluation, and Structure–Activity Relationships of N-Benzoyl-2-hydroxybenzamides as Agents Active against P. falciparum (K1 strain), Trypanosomes, and Leishmania

  摘要：

  In our efforts to identify novel chemical scaffolds for the development of new antiprotozoal drugs, a compound library was screened against Toxoplasma gondii tachyzoites with activity discovered for N-(4-ethylbenzoyl)-2-hydroxybenzamide la against T. gondii as described elsewhere. Synthesis of a compound set was guided by T. gondii SAR with 1r found to be superior for T. gondii, also active against Thai and Sierra Leone strains of Plasmodium falciparum, and with superior ADMET properties as described elsewhere. Herein, synthesis methods and details of the chemical analysis of the compounds in this series are described. Further, this series of N-benzoyl-2-hydroxybenzamides was repurposed for testing against four other protozoan parasites: Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and P. falciparum (K1 isolate). Structure-activity analyses led to the identification of compounds in this set with excellent antileishmanial activity (compound 1d). Overall, compound 1r was the best and had activity 21-fold superior to that of the standard antimalarial drug chloroquine against the K1 P. falciparum isolate.

  DOI：

  10.1021/jm2015183

文献信息

• EP2301995A1
  申请人：——

  公开号：EP2301995A1

  公开（公告）日：2011-03-30
• Novel therapeutic target for protozoal diseases
  申请人：Rathore Dharmender

  公开号：US20070148185A1

  公开（公告）日：2007-06-28

  A novel Hemozoin Detoxification Protein (HDP) from Plasmodium and related parasites is provided as a target for therapeutic intervention in diseases caused by the parasites. HDP has been shown to play a critical role in adhesion to, or invasion into, host cells by the parasite. Furthermore, HDP catalyzes the neutralization of heme by the parasite, by promoting its polymerization into hemozoin. This invention provides methods and compositions for therapies based on the administration of protein, DNA or cell-based vaccines and/or antibodies based on HDP, or antigenic epitopes of HDP, either alone or in combination with other parasite antigens. Methods for the development and use of compounds that inhibit the catalytic activity of HDP, and diagnostic and laboratory methods utilizing HDP are also provided. HDP is also referred to herein as Fasciclin Related Adhesive Protein (FRAP).
• POLYCARBONATE RESIN COMPOSITION CONTAINING TRIAZINE COMPOUND AND MOLDED ARTICLE USING THE SAME
  申请人：Kitagawa Takashi

  公开号：US20110077331A1

  公开（公告）日：2011-03-31

  A polycarbonate resin composition comprising a compound represented by the following formula (1): wherein each of R 1a , R 1b , R 1c , R 1d and R 1e independently represents a hydrogen atom or a monovalent substituent provided that OH is excluded, at least one of the substituents represents a substituent having a Hammett's σp value of 0.3 or more, and the substituents may be combined each other to form a ring; and each of R 1g , R 1h , R 1i , R 1j , R 1k , R 1m , R 1n and R 1p independently represents a hydrogen atom or a monovalent substituent, and the substituents may be combined each other to form a ring.
• US8748520B2
  申请人：——

  公开号：US8748520B2

  公开（公告）日：2014-06-10
• US8957140B2
  申请人：——

  公开号：US8957140B2

  公开（公告）日：2015-02-17