Synthesis, biological evaluation and docking study of N-(2-(3,4,5-trimethoxybenzyl)benzoxazole-5-yl) benzamide derivatives as selective COX-2 inhibitor and anti-inflammatory agents
[Display omitted] •Synthesis of new N-(2-(3,4,5-trimethoxybenzyl)benzoxazole-5-yl)benzamide derivatives.•In vitro biological evaluation of compounds by COX-2 enzymatic inhibition assay.•In vivo biological evaluation and their histopathological studies.•In silico study by molecular docking of ligands...
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Veröffentlicht in: | Bioorganic chemistry 2018-12, Vol.81, p.191-202 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | eng |
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•Synthesis of new N-(2-(3,4,5-trimethoxybenzyl)benzoxazole-5-yl)benzamide derivatives.•In vitro biological evaluation of compounds by COX-2 enzymatic inhibition assay.•In vivo biological evaluation and their histopathological studies.•In silico study by molecular docking of ligands using crystal structure of COX-2.•Compounds 3b, 3d, 3l and 3m showed most promising activity.
A series of N-(2-(3,4,5-trimethoxybenzyl)-benzoxazole-5-yl)benzamide derivatives (3a–3n) was synthesized and evaluated for its in vitro inhibitory activity against COX-1 and COX-2. The compounds with considerable in vitro activity (IC50 |
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ISSN: | 0045-2068 1090-2120 |
DOI: | 10.1016/j.bioorg.2018.07.007 |