Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents

A series of novel monosubstituted sulfonylurea derivatives 10a–y were synthesized and characterized by 1H NMR, 13C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20–100 mg/L. Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC50 against THP-1 cells greater than 100 mg/L.

Graphical abstractA series of novel monosubstituted sulfonylurea derivatives were synthesized and evaluated for their antituberculosis activities. Compounds 10b and 10o displayed potent activities against clinical MDR and XDR TB.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► A series of 25 novel monosubstituted sulfonylurea derivatives were synthesized. ► Five novel compounds showed potent antituberculosis activities in vitro. ► 10b and 10o displayed potent activities in vitro against clinical MDR and XDR TB.