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Table 1 Activity of N-substituted analogs of the PIP series against M. tuberculosis

From: The 4-aminopiperidine series has limited anti-tubercular and anti-staphylococcus aureus activity

Compound

R-group

Mtb. MICa(μM)

% Ib

TC50c(μM)

Staphylococcus aureus IC90(μM)

1

10

-

28

>200

2

H

>20

<30

14

>200

3

20

-

1.8

ND

4

>20

<30

31

ND

5

>20

<30

21

ND

6

>20

74

12.5

ND

7

>20

<30

71

>200

8

>20

<30

66

ND

9

>20

<30

13

ND

10

>20

<30

80

ND

11

>20

<30

>100

ND

  1. aMtb. MIC is the minimum concentration required to inhibit growth of M. tuberculosis completely in liquid culture. MIC is the average of two independent experiments; b% inhibition of growth at 20 μM for compounds with MIC >20 μM.
  2. ND: not determined; cTC50 is the concentration required to inhibit growth of Vero cell line by 50%. TC50 is the average of two independent experiments.