Synthesis and antimicrobial activity of pyrimidine chalcones

被引:20
作者
Kumar, Rakesh [1 ]
Arora, Jyoti [1 ,2 ]
Prasad, Ashok K. [2 ]
Islam, Najmul [3 ]
Verma, Anita K. [3 ]
机构
[1] Univ Delhi, Dept Chem, Kirori Mal Coll, Delhi 110007, India
[2] Univ Delhi, Dept Chem, Bioorgan Lab, Delhi 110007, India
[3] Univ Delhi, Dept Zool, Kirori Mal Coll, Nanotechnol Lab, Delhi 110007, India
关键词
Barbituric acid; Triazole; Chalcone; Antimicrobial activity; CLICK CHEMISTRY; ANTIBACTERIAL ACTIVITY; INHIBITORS; 1,2,3-TRIAZOLES; PROTEASE; DESIGN;
D O I
10.1007/s00044-013-0555-y
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In the realm of biochemical research, chalcones have been efficiently explored as antimicrobial agents. The present study focuses on the synthesis of pyrimidine chalcones, i.e. (E)-1-(6'-hydroxy-1',3'-dimethyl-1',2',3',4'-tetrahydro-2',4'-dioxopyrimidin-5'-yl)-3-[-p-{(1aEuro(3)-aryl-1H-1aEuro(3),2aEuro(3),3aEuro(3)-triazol-4aEuro(3)-yl) methoxy}phenyl]-prop-2-ene-1-ones (7a-7i) by the reaction of 4-triazolomethoxybenzaldehyde, i.e. 4-{(1-aryl-1H-1,2,3-triazol-4-yl)methoxy}benzaldehyde (4a-4i) and 5-acetyl-1,3-dimethylbarbituric acid in (6) 50-80 % yields. The structures of these compounds were established on the basis of their FT-IR, H-1 NMR, C-13 NMR and mass spectral analysis. Compounds 7b-7i were screened for their in vitro antibacterial activity against Rhodococcus rhodochrous MTCC 265, a gram +ve bacteria and Escherichia coli, a gram -ve bacteria by the agar disc diffusion method.
引用
收藏
页码:5624 / 5631
页数:8
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