1385766-80-2Relevant academic research and scientific papers
1,2,3-Triazole derivatives as antitubercular agents: synthesis, biological evaluation and molecular docking study
Shaikh, Mubarak H.,Subhedar, Dnyaneshwar D.,Nawale, Laxman,Sarkar, Dhiman,Kalam Khan, Firoz A.,Sangshetti, Jaiprakash N.,Shingate, Bapurao B.
, p. 1104 - 1116 (2015/06/25)
Searching for new active molecules against Mycobacterium tuberculosis (MTB) H37Ra, a small focused library of 1,2,3-triazoles has been efficiently prepared via a click chemistry approach. The newly synthesized compounds were tested against drug-sensitive MTB. Several derivatives were found to be promising inhibitors of MTB characterized by lower MIC values (5.8-29.9 μg mL-1). Among all the synthesized 31 compounds, 15e was the most active compound against MTB. Based on the results from the anti-tubercular activity, SAR for the synthesized series has been developed. The active compounds from the anti-tubercular study were further tested for anti-proliferative activity against THP-1, A549 and PANC-1 cell lines using MTT assay and showed no significant cytotoxic activity against these three cell lines except THP-1 at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antioxidant activities with an IC50 range of 10.1-37.3 μg mL-1. The molecular docking study of the synthesized compounds was performed against the DprE1 enzyme of MTB to understand the binding interactions. Moreover, the synthesized compounds were also analysed for ADME properties and all the experimental results promote us to consider this series as a starting point for the development of novel and more potent anti-tubercular agents in the future.
Metallic copper wire: a simple, clear and reusable catalyst for the CuAAC reaction in supercritical carbon dioxide
Jiang, Yuqin,He, Xing,Zhang, Weiwei,Li, Xingfeng,Guo, Niu,Zhao, Yaru,Xu, Guiqing,Li, Wei
, p. 73340 - 73345 (2015/09/15)
An efficient protocol for the CuAAC reaction catalyzed by metallic copper wire for the synthesis of 1,4-disubstituted triazoles has been developed in supercritical carbon dioxide (scCO2) at 50 °C. The protocol could afford the corresponding pro
Carboxymethylpullulan promoted Cu2O-catalyzed Huisgen-click reaction
Zhang, Weiwei,Ren, Baoqi,Jiang, Yuqin,Hu, Zhiguo
, p. 12043 - 12047 (2015/02/19)
A combination of carboxymethylpullulan (CMP) and Cu2O has been developed as a highly efficient catalytic system for the Huisgen-click reaction. Our results indicate that the acidic CMP could be used for 6 cycles without decreasing the activatin
A simple, efficient thermally promoted protocol for Huisgen-click reaction catalyzed by CuSO4·5H2O in water
Jiang, Yuqin,Kong, Duanyang,Zhao, Jinglin,Zhang, Weiwei,Xu, Wenjing,Li, Wei,Xu, Guiqing
supporting information, p. 2410 - 2414 (2014/05/06)
A thermally promoted and CuSO4-catalyzed new version of the Huisgen-click reaction is presented in this Letter. Notably, this protocol was suitable not only for the reactions between organic azides and alkynes, but also for one-pot three-component reactions among alkyl halides, NaN3, and alkynes.
Cu(OAc)2·H2O/NH2NH 2·H2O: An efficient catalyst system that in situ generates Cu2O nanoparticles and HOAc for Huisgen click reactions
Jiang, Yuqin,Kong, Duanyang,Zhao, Jinglin,Qi, Qinghua,Li, Wei,Xu, Guiqing
, p. 1010 - 1014 (2014/01/06)
A combination of Cu(OAc)2·H2O and NH 2NH2·H2O, which in situ generates Cu2O-NPs and HOAc in water at room temperature, has been developed as a highly efficient catalytic system for Huisgen
An efficient synthesis of 1,4-disubstituted triazoles in water via CuCl2/Zn-catalyzed huisgen cycloaddition
Jiang, Yuqin,Zhang, Peng,Li, Wei,Li, Xiaojing,Xu, Guiqing
experimental part, p. 226 - 230 (2012/06/30)
An efficient method for the synthesis of 1,4-disubstituted triazoles in water at room temperature has been developed using CuCl2/Zn as a catalyst system. Under the optimized conditions, a novel series of 1,4-disubstituted 1,2,3-triazoles were synthesized.
