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. 2023 Dec 29;67(1):81–109. doi: 10.1021/acs.jmedchem.3c00925

Table 5. In Vitro Antimycobacterial Activities of the Tetrazole-Based Compounds 66ae and 67ae with 3,4-Dinitrobenzyl and 2,5-Dinitrobenzyl Groups, Respectively, and Trifluoromethyl Analogues of the Latter with 5-Trifluoromethyl and 2-Trifluoromethyl Groups 70ae and 71ae, Respectively, Expressed as MIC (μM) and Their Comparison with Those of Parent Tetrazoles 1ae12.

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  X M. tuberculosis My 331/88a M. avium My 330/88a M. kansasii My 235/80b
INH   0.5/1 250/250 250/250/250
pretomanid   0.125/0.25 >32/>32 >32/>32/>32
1a 3-NO2 4/4 62/62 2/4/16
1b 3-NO2 2/4 16/32 1/4/4
1c 3-NO2 1/2 125/125 2/4/4
1d 3-NO2 1/1 125/125 1/2/2
1e 3-NO2 1/1 16/32 4/4/4
66a 4-NO2 16/16 32/32 16/32/32
66b 4-NO2 32/32 125/125 16/32/32
66c 4-NO2 4/8 250/250 2/4/8
66d 4-NO2 16/16 250/250 8/16/16
66e 4-NO2 32/64 >1000/>1000 32/64/125
67a 2-NO2 1/1 250/250 2/4/4
67b 2-NO2 0.5/1 250/250 1/1/1
67c 2-NO2 0.5/1 250/250 1/1/2
67d 2-NO2 1/1 250/250 1/1/2
67e 2-NO2 1/1 250/250 1/1/1
70a - 250/250 250/250 125/250/250
70b70e - 250/250 250/250 250/250/250
71a 2-CF3 32/32 250/250 64/132/250
71b 2-CF3 8/8 250/250 32/32/32
71c 2-CF3 250/250 250/250 250/250/250
71d 2-CF3 250/250 250/250 250/250/250
71e 2-CF3 32/32 250/250 64/64/64
a

14/21 days.

b

7/14/21 days.