Table 2 Identification of common targets or mechanisms of resistance.

From: Novel chemical entities inhibiting Mycobacterium tuberculosis growth identified by phenotypic high-throughput screening

Chemotype

Molecule

Wild-type

MmpL3 F255L

Fold change

Structure

IC90 (µM)

IC90 (µM)

4-phenylpiperidine

4PP-1

6.3

68

11

See Fig. 2

4-phenylpiperidine

4PP-31

2.7

45

15

See Table 3

4-phenylpiperidine

4PP-44

5.2

18

3.5

See Table 3

Aminopyridylpyrimidine

APDP-1

10

9.2

0.9

See Fig. 2

Aminopyridylpyrimidine

APDP-2

33

15

0.5

See Fig. 3

Aminopyridylpyrimidine

APDP-3

6.3

22

3.5

See Fig. 3

Hydrophobic urea

HBU-1

4.2

6

1.4

See Fig. 2

Hydrophobic urea

HBU-2

4.9

39

8.0

See Fig. 3

Hydrophobic urea

HBU-3

29

71.0

2.4

See Fig. 3

Hydrophobic urea

HBU-4

12

> 100

> 8.3

See Fig. 3

Hydrophobic urea

HBU-5

13

6.9

0.5

See Fig. 3

Pyrazolylpyrimidines

PZP-1

5.2

> 100

> 19

See Fig. 3

Pyrazolylpyrimidines

PZP-2

7.4

> 100

> 13

See Fig. 3

Pyrazolylpyrimidines

PZP-3

4.5

46

10

See Fig. 2

Chemotype

Molecule

Wild-type

QcrB A396T

Fold-change

Structure

IC90 (µM)

IC90 (µM)

Pyrrolotriazines

PYT

11

62

5.8

See Fig. 2

Thienylpyrazolylthiazoles

TPT

7.1

63

8.9

See Fig. 2

  1. We determined the MIC against wild-type M. tuberculosis and strains with mutations in either MmpL3 or QcrB. The fold change with respect to the wild-type MIC; in bold if change > three-fold. Structures are shown in Figs. 2 and 3.
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