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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 1.

Inhibition of Mtb and Yp Dxr by selected N-acyl and O-linked MEPicides

graphic file with name nihms835585t1.jpg
Cmpd No. R1 R2 Mtb Dxr
IC50, µM
Yp Dxr
IC50, µM
1 (Fos) H H 0.44 0.71
2 (FR) H CH3 2.91 0.23
8b H Hexyl (43)* (27)
8e H Ph (70) 4.45
8f H (4-CH3)Ph (74) 16.03
8h H CH2CH2CH2Ph 17.8 (34)
16d (4-ipr)Bn CH3 48.4 1.19
16e CH(CH3)Ph CH3 (38.1) (19)
16g CH2CH2(4-OH)Ph CH3 (59) (22)
16i CH2-(1-naphthyl) CH3 (29) 22.35
16j CH2-(2-naphthyl) CH3 1.45 0.33
16k CH2-4-(1,1’-biphenyl) CH3 (36.8) 8.40
16r CH2-4-(4’-CF3)-1,1’-biphenyl) CH3 (70) (19)
*

Values in parentheses are percent remaining enzyme activity at 100 µM.