Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2) was written by Tan, Li;Nomanbhoy, Tyzoon;Gurbani, Deepak;Patricelli, Matthew;Hunter, John;Geng, Jiefei;Herhaus, Lina;Zhang, Jianming;Pauls, Eduardo;Ham, Youngjin;Choi, Hwan Geun;Xie, Ting;Deng, Xianming;Buhrlage, Sara J.;Sim, Taebo;Cohen, Philip;Sapkota, Gopal;Westover, Kenneth D.;Gray, Nathanael S.. And the article was included in Journal of Medicinal Chemistry in 2015.Application In Synthesis of 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:
The authors developed a pharmacophore model for type II inhibitors that was used to guide the construction of a library of kinase inhibitors. Kinome-wide selectivity profiling of the library resulted in the identification of a series of 4-substituted 1H-pyrrolo[2,3-b]pyridines that exhibited potent inhibitory activity against two mitogen-activated protein kinases (MAPKs), TAK1 (MAP3K7) and MAP4K2, as well as pharmacol. well interrogated kinases such as p38α (MAPK14) and ABL. Further investigation of the structure-activity relationship (SAR) resulted in the identification effect two potent dual TAK1 and MAP4K2 inhibitors such as I as well as two MAP4K2 selective inhibitors such as II. Some of these inhibitors possess good pharmacokinetic properties that will enable their use in pharmacol. studies in vivo. A 2.4 Å cocrystal structure of TAK1 in complex with 1 confirms that the activation loop of TAK1 assumes the DFG-out conformation characteristic of type II inhibitors. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Application In Synthesis of 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).
4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Application In Synthesis of 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics