Full
Outline
To obtain a series of multi-target inhibitors with better anti-inflammatory activity by using 1-benzoyl-4-(phenoxyacetyl) piperazine as the lead compound followed by further structure optimization.
Substituted benzoic acid was used as a starting material, and 18 target compounds were synthesized through substitution and acylation reactions. The inhibitory effects of all compounds on lipopolysaccharide (LPS)-induced tumor necrosis factor (TNF)-α and interleukin (IL)-6 secretion in RAW264.7 cells were measured, and molecular docking was performed on the compounds with better anti-inflammatory activity.
The structures of all the compounds were confirmed by 1H NMR, 13C NMR and HRMS. Compounds 3d and 8k demonstrated better inhibitory activity on TNF-α secretion, and compounds 3b and 3d showed better inhibitory activity on IL-6 secretion.
Compound 3d has good inhibitory activity on TNF-α and IL-6 secretion in RAW264.7 cells induced by LPS, and is worthy of further study.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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