111098-19-2Relevant academic research and scientific papers
RSK2 benzo triazole derivatives as inhibitors of synthesis and use
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Paragraph 0078-0080, (2016/10/07)
The invention relates to synthesis of a benzotriazol derivative and its application, specifically to a compound as shown in the following formula II, a pharmaceutical composition containing the compound as shown in the formula II and an application of the compound in preparation of drugs for treating or preventing RSK2-mediated diseases.
Triazole and benzotriazole derivatives as novel inhibitors for p90 ribosomal S6 protein kinase 2: Synthesis, molecular docking and SAR analysis
Yuan, Jun,Zhong, Ye,Li, Shiliang,Zhao, Xue,Luan, Guoqin,Zhao, Zhenjiang,Huang, Jin,Li, Honglin,Xu, Yufang
, p. 1192 - 1198 (2013/10/21)
A series of triazole and benzotriazole derivatives as novel p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors were designed and synthesized. The in vitro activities against RSK2 were evaluated, and among 14 compounds, compounds 5, 6, 11, 12, 13 and 14 exhibited enzyme IC50 values of 8.91, 2.86, 3.19, 3.05, 4.49 and 2.09 μmol/L respectively. The proposed binding modes were simulated using molecular docking method, and the docking results coupled with the structure-activity relationship (SAR) analysis indicated that all these active compounds bound to the RSK2 ATP binding site at NTKD, and the electron-donating groups on the 4-position of phenyl were the determinant point for the inhibitory activity. In the present study, a series of triazole and benzotriazole derivatives as novel p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors were designed and synthesized. The in vitro activities of the 14 compounds against RSK2 were evaluated, among which, compounds 5, 6, 11, 12, 13 and 14 exhibited enzyme IC50 values of 8.91, 2.86, 3.19, 3.05, 4.49 and 2.09 μmol/L respectively. The proposed binding modes were simulated using molecular docking method, and the docking results coupled with the structure-activity relationship (SAR) analysis indicated that all our active compounds bound to the RSK2 ATP binding site at NTKD, and the electron-donating groups on the 4-position of phenyl were the key point for the inhibitory activity. Copyright
Simple and convenient preparation of 1-(arylamino)methylbenzotriazoles and -(arylamino)methylbenzimidazoles
Milata,Kada,Zalibera,Belicova
, p. 215 - 220 (2007/10/03)
The preparation of 1-(arylamino)methylbenzotriazoles 1a-17a and benzimidazoles 1b-17b is described and their antibacterial activity evaluated. 1-Hydroxymethylbenzazoles react with the appropriate aniline to yield the target compounds. These were characterized using 1H NMR, IR, UV spectra. The compounds displayed no significant antibacterial activity.
The Chemistry of Benzotriazole. Part 3. The Aminoalkylation of Benzotriazole
Katritzky, Alan R.,Rachwal, Stanislaw,Rachwal, Bogumila
, p. 799 - 804 (2007/10/02)
1-(1-Hydroxyalkyl)benzotriazoles convert a wide variety of aromatic and heteroaromatic primary amines into their mono N- derivatives in high yield.Aliphatic primary amines frequently give bis-derivatives.Product structure is established by 13C n.m.r.; dangers in the use of 1H n.m.r. to distinguish 1- and 2-substituted benzotriazoles are pointed out.
