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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.