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Literature summary for 1.4.1.1 extracted from

  • Saxena, S.; Samala, G.; Sridevi, J.P.; Devi, P.B.; Yogeeswari, P.; Sriram, D.
    Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors (2015), Eur. J. Med. Chem., 92, 401-414 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
5-(4-(benzyloxy)benzylidene)-3-(2,5-dimethylphenyl)-2-iminothiazolidin-4-one compound shows potency, selectivity, and no cytotoxicity up to 50 microM in a mouse macrophage cell line Mycobacterium tuberculosis
5-(4-(benzyloxy)benzylidene)-3-(2,6-dimethylphenyl)-2-iminothiazolidin-4-one compound shows potency, selectivity, and no cytotoxicity up to 50 microM in a mouse macrophage cell line Mycobacterium tuberculosis
6-acetyl-2-(4-chlorobenzamido)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxamide compound shows potency, selectivity, and no cytotoxicity up to 50 microM in a mouse macrophage cell line Mycobacterium tuberculosis
tert-butyl 3-carbamoyl-2-(4-chlorobenzamido)-4,5-dihydrothieno[2,3-c]pyridine-6(7H)-carboxylate compound shows potency, selectivity, and no cytotoxicity up to 50 microM in a mouse macrophage cell line Mycobacterium tuberculosis

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.049
-
L-alanine pH 10.2, 37°C Mycobacterium tuberculosis
0.53
-
NAD+ pH 10.2, 37°C Mycobacterium tuberculosis

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WQB1
-
-
Mycobacterium tuberculosis H37Rv P9WQB1
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-alanine + H2O + NAD+
-
Mycobacterium tuberculosis pyruvate + NH3 + NADH + H+
-
?
L-alanine + H2O + NAD+
-
Mycobacterium tuberculosis H37Rv pyruvate + NH3 + NADH + H+
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00058
-
pH 10.2, 37°C Mycobacterium tuberculosis tert-butyl 3-carbamoyl-2-(4-chlorobenzamido)-4,5-dihydrothieno[2,3-c]pyridine-6(7H)-carboxylate
0.00064
-
pH 10.2, 37°C Mycobacterium tuberculosis 6-acetyl-2-(4-chlorobenzamido)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxamide
0.00134
-
pH 10.2, 37°C Mycobacterium tuberculosis 5-(4-(benzyloxy)benzylidene)-3-(2,5-dimethylphenyl)-2-iminothiazolidin-4-one
0.00174
-
pH 10.2, 37°C Mycobacterium tuberculosis 5-(4-(benzyloxy)benzylidene)-3-(2,6-dimethylphenyl)-2-iminothiazolidin-4-one