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. 2024 Jan 15;98:129596. doi: 10.1016/j.bmcl.2023.129596

Table 3.

In vitro anti-TB inhibitory activity and cytotoxicity of aryl fluorosulfate 3i, 20a-20 l, and 21a-21f

graphic file with name fx37.jpg

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compound R1 R2 Anti-TB activity
 Cytotoxicity
H37Rv MIC (µM) HEK293T CC50 (µM) HepG2 CC50 (µM)
3i H H 0.6 >40 5.8
20a H Me 0.3 17.1 16.3
20b H Et 0.6 >40 5.8
20c H iPr 0.6 16.7 12.4
20d H tBu 1.2 13.7 6.9
20e Me Me 0.23 14.3 8.1
20f H OMe 0.6 >40 >40
20 g H CN 0.45 ND 10.3
20 h H N(Me)2 0.31 >40 >40
20i H SO2Me 0.40 17.2 9.3
20j H COOH 1.25 >40 >40
20 k H CONH2 0.17 >40 >40
21a H NHCOMe 0.15 >40 >40
21b H NHSO2Me 0.06 >40 >40
20 l H SONH2 0.47 ND >40
21c H N(Me)SO2Me 0.31 ND 15.3
21d H NHSO2Et 0.08 ND >40
21e H NHSO2iPr 0.31 >40 >40
21f H NHSO2tBu 2.5 >40 >40