Table 3.
Cpd. No. |
R1 | R2 | R3 | R4 | R5 | R6 | R7 | TB IC90 |
SI |
---|---|---|---|---|---|---|---|---|---|
2a | H | Ph | H | H | H | cC6H11 | H | 0.18 | >83 |
2b | H | 3-nitro phenyl |
H | H | H | i-Pr | H | 0.45 | >33 |
2c | H | n-butyl | H | Cl | H | Et | Me | 0.64 | >23 |
2d | H | n-butyl | H | Cl | H | CH2Ph | H | 0.66 | >23 |
2e | H | 3-nitro phenyl |
H | H | H | Me | H | 0.78 | >19 |
2f | CH2CO2Me | Me | H | H | Me | CH2Ph | H | 1.03 | >15 |
2g | H | 4- methoxy phenyl |
H | H | H | H | 1.7 | >9 | |
2h | Et | Me | H | H | Me | Me | H | 1.8 | >8 |
2i | 2- benzothiazolyl |
H | H | H | H | Et | H | 2.7 | >6 |
2j | -(CH2)5- | H | H | H | Et | H | 3.5 | >4 | |
2k | Cl | CH3 | OCH2CO2Me | H | H | Me | H | Inact. | - |
2l | -(CH2)3)- | H | H | H | Me | Ph | * | - |
58% Inhibition in our initial single dose assay, not evaluated in the dose response assay.