Synthesis, Antibacterial Activity, and Docking Studies of 1,2,3-triazole-tagged Thieno[2,3-d]pyrimidinone Derivatives

被引:15
|
作者
Kumari, M. Aruna [1 ]
Triloknadh, S. [1 ]
Harikrishna, N. [1 ]
Vijjulatha, M. [2 ]
Rao, C. Venkata [1 ]
机构
[1] Sri Venkateswara Univ, Dept Chem, Tirupati 517502, Andhra Pradesh, India
[2] Osmania Univ, Dept Chem, Univ Coll Sci, Telangana, India
关键词
BIOLOGICAL EVALUATION; TERMINAL ALKYNES; TRIAZOLE; DESIGN; AGENTS; THIENOPYRIMIDINE; CYCLOADDITION; AZIDES;
D O I
10.1002/jhet.2995
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Novel (1-(substituted phenyl)-1H-1,2,3-triazol-4-yl)methyl-2-(4-oxo-5,6,7,8-tetrahydrobenzo[1,2]thieno[2,3-d]pyrimidin-3(4H)-yl)acetate derivatives were synthesized. All the compounds showed significant antibacterial activity against Gram-negative (Escherichia coli and Klebsiella pneumonia) and Gram-positive (Bacillus subtilis and Bacillus cereus) bacteria. Particularly, (1-(3-nitrophenyl)-1H-1,2,3-triazol-4-yl) methyl-2-(4-oxo-5,6,7,8-tetrahydrobenzo[1, 2] thieno[2,3-d] pyrimidin-3(4H)-yl) acetate was found to be most potent against E. coli, K. pneumonia, and B. subtilis with MIC 25 mu g/ml. Molecular docking was also performed on purine riboswitch of B. subtilis and thiamine pyrophosphate riboswitch of E. coli.
引用
收藏
页码:3672 / 3681
页数:10
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