Modifying tetramethyl–nitrophenyl–imidazoline with amino acids: design, synthesis, and 3D-QSAR for improving inflammatory pain therapy

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ID: 48842
2015
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Abstract
Xueyun Jiang,1 Yuji Wang,1 Haimei Zhu,1 Yaonan Wang,1 Ming Zhao,1,2 Shurui Zhao,1 Jianhui Wu,1 Shan Li,1 Shiqi Peng11Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China; 2Faculty of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung, TaiwanAbstract: With the help of pharmacophore analysis and docking investigation, 15 novel 1-(4,4,5,5-tetramethyl-2-(3-nitrophenyl)-4,5-dihydroimidazol-1-yl)-oxyacetyl-L-amino acids (6a–o) were designed, synthesized, and assayed. On tail-flick and xylene-induced ear edema models, 10 µmol/kg 6a–o exhibited excellent oral anti-inflammation and analgesic activity. The dose-dependent assay of their representative 6f indicates that the effective dose should be 3.3 µmol/kg. The correlation of the three-dimensional quantitative structure–activity relationship with the docking analysis provides a basis for the rational design of drugs to treat inflammatory pain.Keywords: tetramethylimidazoline, analgesic, anti-inflammatory, 3D-QSAR
Reference Key
x2015modifyingdrug Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors X, Jiang;Y, Wang;H, Zhu;Y, Wang;M, Zhao;S, Zhao;J, Wu;S, Li;S, Peng;
Journal Drug design, development and therapy
Year 2015
DOI
DOI not found
URL
http://www.dovepress.com/modifying-tetramethylndashnitrophenylndashimidazoline-with-amino-acids-peer-reviewed-article-DDDT
Keywords
chemistry Therapeutics. Pharmacology Medicine Materials of engineering and construction. Mechanics of materials Technology Science physics environmental sciences chemical engineering genetics environmental technology. sanitary engineering industrial medicine. industrial hygiene

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