Synthesis of novel isoflavone/benzo-δ-sultam hybrids as potential anti-inflammatory drugs

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Abstract

A small series of novel isoflavone/benzo-δ-sultam hybrids was synthesised and evaluated as potential anti-inflammatory and neuroprotective drugs in LPS-activated BV2 microglia. The benzo-δ-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-α 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-α to 34% at 20 µM final concentration in the well.

Original languageEnglish
Article number127761
Number of pages8
JournalBioorganic and Medicinal Chemistry Letters
Volume34
Early online date24 Dec 2020
DOIs
Publication statusPublished - 15 Feb 2021

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