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. Author manuscript; available in PMC: 2017 Dec 9.
Published in final edited form as: ACS Infect Dis. 2016 Oct 12;2(12):923–935. doi: 10.1021/acsinfecdis.6b00125

Table 2.

Antitubercular activities of saturated acid and ester MEPicides

graphic file with name nihms835585t2.jpg
Cmpd No. R1 R2 R3 M. tuberculosis
MIC (µg/mL)*
INH N/A N/A N/A 0.01
1 (Fos) H H H/Na >500
2 (FR900098) H CH3 H/Na >500
3 H CH3 CH2OCOtBu 50–100 (62.5)
8e H Ph H/Na ≥200
8h H (CH2)3Ph H/Na >200
7h H (CH2)3Ph CH2CH3 200
12 H (CH2)3Ph CH2OCOtBu 150
8d H (CH2)2cyclohexyl H/Na >200 (25)
7d H (CH2)2cyclohexyl CH2CH3 >200 (37)
8l H CH2O(4-Cl)Ph H/Na >200 (25)
16d (4-ipr)Bn CH3 H/Na 200 (25)
17 (4-ipr)Bn CH3 CH2OCOtBu 12.5 (6.25–12.5)
16k CH2-4-(1,1’-biphenyl) CH3 H/Na 25–50
15k CH2-4-(1,1’-biphenyl) CH3 CH2CH3 200 (100)
19 CH2-4-(1,1’-biphenyl) CH3 CH2OCOtBu 12.5 (3.13–6.25)
16p CH2-4-(4’-ipr)-1,1’-biphenyl CH3 H/Na 100 (6.25–12.5)
16h (CH2)4Ph CH3 H/Na ≥200
15h (CH2)4Ph CH3 CH2CH3 100–200
21 (CH2)4Ph CH3 CH2OCOPh 25
18 (CH2)4Ph CH3 CH2OCOtBu 12.5 (6.25–12.5)
16j CH2-(2-naphthyl) CH3 H/Na ≥200
15j CH2-(2-naphthyl) CH3 CH2CH3 200 (100)
20 CH2-(2-naphthyl) CH3 CH2OCOtBu 18.75 (4.7)
*

Data using 7H9 media. When different, MIC in GAST-Fe media is given in parentheses.