期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 102, 期 -, 页码 631-638出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.08.025
关键词
N2-(arylacetyl)glycinanilide; TyrRS inhibitor; Antibacterial agent; Molecular docking; Structure-activity relationship
资金
- National Natural Science Foundation of China [21262013]
- Hunan Provincial Natural Science Foundation of China [2015JJ2116]
- Science and Technology Innovative Research Team in Jishou University for Improving Drug-like Properties of Active Components from Medicinal Plants in Wulin Montains
Tyrosyl-tRNA synthetase (TyrRS), an essential enzyme in bacterial protein biosynthesis, is an attractive therapeutic target for finding novel antibacterial agents, and a series of N2-(arylacetyl)glycinanilides has been herein synthesized and identified as TyrRS inhibitors. These efforts yielded several compounds, with IC50 in the low micromolar range against TyrRS from Staphylococcus aureus. Out of the obtained compounds, 3ap is the most active and exhibits excellent activity against both Gram-positive (S. aureus) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacterial strains. In comparison with the parent scaffold 3-arylfuran-2(5H)-one, N2-(arylacetyl)glycinanilide significantly improved the potency against Gram-negative bacterial strains, indicating that this scaffold offers a significant potential for developing new antibacterial drugs. (C) 2015 Elsevier Masson SAS. All rights reserved.
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