期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 34, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127761
关键词
Isoflavone; delta-sultam; Anti-inflammatory; Microglia; TNF-alpha
资金
- University of Huddersfield
A series of novel isoflavone/benzo-o-sultam hybrids were synthesized and evaluated for their potential anti-inflammatory and neuroprotective effects in LPS-activated BV2 microglia. The most potent hybrid compound showed promising results by reducing NO production to 41% and TNF-alpha to 34% in the cells.
A small series of novel isoflavone/benzo-o-sultam hybrids was synthesised and evaluated as potential anti-inflammatory and neuroprotective drugs in LPS-activated BV2 microglia. The benzo-o-sultam core was constructed in a two-step reaction by coupling 2-halobenzenesulfonamide derivatives with terminal alkynes, followed by a 6-endo-dig cyclisation. The synthesised compounds, including precursors and hybrids, were tested for their ability to inhibit NO and TNF-alpha production in LPS-stimulated BV2 microglial cells, and the results are promising. The most potent hybrid reduces the NO production to 41%, and the TNF-alpha to 34% at 20 mu M final concentration in the well.
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