A Simple Work-Up-free, Solvent-free Approach to Novel Amino Acid Linked 1,4-Disubstituted 1,2,3-Triazoles as Potent Antituberculosis Agents

被引:37
作者
Garg, Anirban [1 ]
Borah, Debajit [2 ]
Trivedi, Priyanka [3 ]
Gogoi, Dipshikha [4 ]
Chaliha, Amrita Kashyap [4 ]
Ali, Abdul Aziz [1 ,5 ]
Chetia, Dipak [6 ]
Chaturvedi, Vinita [3 ]
Sarma, Diganta [1 ]
机构
[1] Dibrugarh Univ, Dept Chem, Dibrugarh 786004, Assam, India
[2] Royal Global Univ, Dept Biotechnol, Gauhati 395781035, Assam, India
[3] Cent Drug Res Inst, CSIR, Biochem Div, Lucknow 226001, Uttar Pradesh, India
[4] Dibrugarh Univ, Ctr Biotechnol & Bioinformat, Dibrugarh 786004, Assam, India
[5] CSIR NEIST, Mat Sci & Technol Div, Jorhat 785006, Assam, India
[6] Dibrugarh Univ, Dept Pharmaceut Sci, Dibrugarh 786004, Assam, India
关键词
IONIC LIQUIDS; HUISGEN CYCLOADDITION; GROWTH; ROUTE; DPRE1;
D O I
10.1021/acsomega.0c03862
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An efficient, green strategy for synthesis of 1,4-disubstituted-1,2,3-triazole has been developed using 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) acetate ionic liquid (200 mu L) under a solvent- and external base-free condition. This protocol is further applied for the synthesis of novel amino acid containing 1,2,3-triazole molecules, which were then evaluated for potential antitubercular and antibacterial activities. Cytotoxicity assay of the compounds was also performed. In silico analysis of the promising compounds selected through experimental analysis was thereafter performed for visualizing molecular interactions and predicting binding affinities between our synthesized molecules, which exhibited good activity in experimental studies and the DprE1 target protein of Mycobacterium tuberculosis. Durg-likeness studies also show potential of the synthesized molecules as drug candidates.
引用
收藏
页码:29830 / 29837
页数:8
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