88372-33-2Relevant academic research and scientific papers
Application of ethyl benzamide compound to preparation of local anesthetics
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Paragraph 0016-0017; 0019-0020, (2021/02/09)
The invention provides an application of an ethyl benzamide compound to preparation of local anesthetics. The structure of the compound is shown in the following formula, and the compound has the characteristics of small toxic and side effects, short time
Structure-Activity Relationships of Potent, Targeted Covalent Inhibitors That Abolish Both the Transamidation and GTP Binding Activities of Human Tissue Transglutaminase
Akbar, Abdullah,McNeil, Nicole M. R.,Albert, Marie R.,Ta, Viviane,Adhikary, Gautam,Bourgeois, Karine,Eckert, Richard L.,Keillor, Jeffrey W.
, p. 7910 - 7927 (2017/10/06)
Human tissue transglutaminase (hTG2) is a multifunctional enzyme. It is primarily known for its calcium-dependent transamidation activity that leads to formation of an isopeptide bond between glutamine and lysine residues found on the surface of proteins, but it is also a GTP binding protein. Overexpression and unregulated hTG2 activity have been associated with numerous human diseases, including cancer stem cell survival and metastatic phenotype. Herein, we present a series of targeted covalent inhibitors (TCIs) based on our previously reported Cbz-Lys scaffold. From this structure-activity relationship (SAR) study, novel irreversible inhibitors were identified that block the transamidation activity of hTG2 and allosterically abolish its GTP binding ability with a high degree of selectivity and efficiency (kinact/KI > 105 M-1 min-1). One optimized inhibitor (VA4) was also shown to inhibit epidermal cancer stem cell invasion with an EC50 of 3.9 μM, representing a significant improvement over our previously reported "hit" NC9.
Oxazolo[4,5-b]pyridine-Based Piperazinamides as GSK-3β Inhibitors with Potential for Attenuating Inflammation and Suppression of Pro-Inflammatory Mediators
Tantray, Mushtaq A.,Khan, Imran,Hamid, Hinna,Alam, Mohammad Sarwar,Dhulap, Abhijeet,Ganai, Ajaz Ahmad
, (2017/08/07)
Recent studies reveal that glycogen synthase kinase-3β (GSK-3β) acts as a pro-inflammatory enzyme, and by inhibiting this kinase, inflammation can be controlled. In this regard, a series of 17 piperazine-linked oxazolo[4,5-b]pyridine-based derivatives was
Identification and characterization of small molecule modulators of the epstein-barr virus-induced gene 2 (EBI2) receptor
Gessier, Francois,Preuss, Inga,Yin, Hong,Rosenkilde, Mette M.,Laurent, Stephane,Endres, Ralf,Chen, Yu A.,Marsilje, Thomas H.,Seuwen, Klaus,Nguyen, Deborah G.,Sailer, Andreas W.
, p. 3358 - 3368 (2014/05/20)
Oxysterols have recently been identified as natural ligands for a G protein-coupled receptor called EBI2 (aka GPR183) (Nature 2011, 475, 524; 519). EBI2 is highly expressed in immune cells (J. Biol. Chem. 2006, 281, 13199), and its activation has been sho
Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)- 2H-phthalazin-1-ones as potent PARP-1 inhibitors
Wang, Ling-Xiao,Zhou, Xin-Bo,Xiao, Meng-Liang,Jiang, Ning,Liu, Feng,Zhou, Wen-Xia,Wang, Xiao-Kui,Zheng, Zhi-Bing,Li, Song
, p. 3739 - 3743 (2014/09/17)
We have developed a series of substituted 4-(thiophen-2-ylmethyl)-2H- phthalazin-1-ones as potent PARP-1 inhibitors. Preliminary biological evaluation indicated that most compounds possessed inhibitory potencies comparable to, or higher than AZD-2281. Among these compounds, 18q appeared to be the most notable one, which displayed an 8-fold improvement in enzymatic activity compared to AZD-2281. These efforts lay the foundation for our further investigation.
Efficient and continuous monoacylation with superior selectivity of symmetrical diamines in microreactors
Maurya, Ram Awatar,Hoang, Phan Huy,Kim, Dong-Pyo
scheme or table, p. 65 - 68 (2012/03/26)
Efficient and continuous monoacylation of symmetrical diamines performed in microreactors yielded superior selectivity to that predicted by statistical considerations. It is highly valuable that the kinetically controlled product in high yields was achieved without any special catalyst at ambient temperature.
CDI-mediated monoacylation of symmetrical diamines and selective acylation of primary amines of unsymmetrical diamines
Verma, Sanjeev K.,Ghorpade, Ramarao,Pratap, Ajay,Kaushik
, p. 326 - 329 (2012/04/10)
A highly efficient and green protocol for monoacylation of symmetrical diamines and chemoselective acylation of primary amines of unsymmetrical diamines has been developed.
THIENO[2,3-d]PYRIMIDINE COMPOUNDS
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, (2010/11/24)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) wherein A1, A2, A3, A4, A5, A6, A7, A
4-PIPERAZINYLTHIENO [2,3-D] PYRIMIDINE COMPOUNDS AS PLATELET AGGREGATION INHIBITORS
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, (2010/11/24)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) wherein A1 , A2, A3, A4, A5, A6, A7, Asup
4-PIPERAZINOTHIENO [2, 3-D] PYRIMIDINE COMPOUNDS AS PLATELET AGGREGATION INHIBITORS
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, (2010/11/24)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: (I) wherein A1, A2, A3, A4, A5, A6, A7, As
