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In order to make the synthetic route of Thiamidol more efficient and easier to scale up, a new method was developed. The compound 2,4-dihydroxyacetophenone was dissolved in ethyl acetate and brominated with cupric bromide. After bromination, the mixture was filtered to remove cuprous bromide. The obtained ethyl acetate solution containing 2-bromo-1-(2, 4-dihydroxyphenyl) ethanone was directly reacted with (2-methylpropanoyl) thiourea to obtain the precipitate of Thiamidol hydrobromide. The precipitate was neutralized by deacidification and recrystallized to afford Thiamidol with high purity. In addition, in the screening of fertilitypromoting substances, Thiamidol was found to be effective in protecting human sperm from motility loss in vitro. This suggests that it may have potential application in fertility protection and promotion. [ABSTRACT FROM AUTHOR]

The 3C-like protease (also known as Mpro) plays a key role in SARS-CoV-2 replication and has similar substrates across mutant coronaviruses, making it an ideal drug target. We synthesized 19 thiazolidinedione derivatives via the Knoevenagel condensations and Mitsunobu reactions as potential 3C-like protease inhibitors. The activity of these inhibitors is screened in vitro by employing the enzymatic screening model of 3C-like protease using fluorescence resonance energy transfer. Dithiothreitol is included in the enzymatic reaction system to avoid non-specific enzymatic inhibition. Active inhibitors with diverse activity are found in this series of compounds, and two representative inhibitors with potent inhibitory activity are highlighted. [ABSTRACT FROM AUTHOR]