EC Number   |
Inhibitors |
Structure |
|---|
    1.4.1.1 | 1-(isonicotinamido)-N2,N4-bis(benzo[d]thiazol-2-yl)azetidine-2,4-dicarboxamide |
compound shows 100fold reduction in nutrient starved dormant Mycobacterium tuberculosis model and MIC of 11.81 microM in actively replicative Mycobacterium tuberculosis |
   |
| 1.4.1.1 | 1-(isonicotinamido)-N2,N4-bis(benzo[d]thiazol-2-yl)azetidine-2,4-dicarboxamide |
- |
|
| 1.4.1.1 | 1-(isonicotinamido)-N2,N4-bis(phenyl)azetidine-2,4-dicarboxamide |
lead compound for inhibitor screening, involved in hydrophobic interactions with residues Pro242, Val241, Ala176, Leu130, Ile267, Ala179, Ile199 and Ile174 |
|
| 1.4.1.1 | 2,4,6-Trinitrobenzenesulfonic acid |
inactivation follows pseudo first-order kinetics with a 1:1 stoichiometric ratio between the reagent and the enzyme subunit. Partial protection by each of the substrates, NADH or pyruvate. Complete protection only in presence of the ternary complex enzyme-NADH-pyruvate |
|
| 1.4.1.1 | 2-ethyl-N-phenethyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine |
the molecule shows activity against nutrient-starved nonreplicating Mycobacterium tuberculosis, resulting in a 2.7 log reduction of bacterial loads at 0.010 mg/ml, and is shown to be more potent than the first-line antitubercular drugs, isoniazid and rifampicin, at the same dose. compound is cytotoxic |
|
| 1.4.1.1 | 2-oxobutanoate |
weak |
|
| 1.4.1.1 | 3-(2-pyridyldithio)propionate |
inactivation follows pseudo first-order kinetics with a 1:1 stoichiometric ratio between the reagent and the enzyme subunit. Partial protection by each of the substrates, NADH or pyruvate. Complete protection only in presence of the ternary complex enzyme-NADH-pyruvate |
|
| 1.4.1.1 | 3-Bromopyruvate |
- |
|
| 1.4.1.1 | 3-hydroxypyruvate |
competitive with respect to pyruvate |
|
| 1.4.1.1 | 4-(furan-2-ylmethylene)-1-phenylpyrazolidine-3,5-dione |
the compound exhibited potent antitubercular activity against log-phase cultures of Mycobacterium tuberculosis with a MIC of 0.0245 mM, but is found to be less active than the lead compound 1-(4-chlorophenyl)-4-(4-hydroxy-3-methoxy-5-nitrobenzylidene) pyrazolidine-3,5-dione (CD59). The compound is cytotoxic |
|
