High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv

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“…However, the BTD series was also active against eukaryotic cells showing significant toxicity against the Vero cell line; in fact cytotoxicity was more pronounced than the anti-mycobacterial activity. Our data are in contrast to that previously reported in which cytotoxicity was not observed in selected members of the series [3]. Differences in cytotoxicity could be due to the exact assay method and the cell line used; in this case we used the same Vero cell line.…”

“…All of the compounds had significant cytotoxicity, with TC50 values < 0.3 µM, suggesting that these compounds are even more effective against eukaryotic cells ( Table 1). Of the compounds we tested, two had (3a and 3i) 3 . In this study 3a appeared to have a selectivity index (SI) of > 33.…”

Synthesis and anti-tubercular activity of 3-substituted benzothiophene-1,1-dioxides

“…The benzo[b]thiophene-1,1-dioxide (BTD) series was reported to have activity against M. tuberculosis in a phenotypic assay [3]. Fourteen compounds were tested from this series; five of these, all of which had heteroarylthio groups, had some inhibitory activity against M.…”

“…Selectivity index was calculated as MIC/TC50. For published data [3], SI was calculated as IC90/TC50. …”

“…All of the compounds had significant cytotoxicity, with TC50 values < 0.3 µM, suggesting that these compounds are even more effective against eukaryotic cells ( Table 1). Of the compounds we tested, two had PrePrints previously been identified as having anti-tubercular activity (3a and 3i) 3 . In this study 3a appeared to have a selectivity index (SI) of > 33.…”