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Literature summary for 1.3.1.9 extracted from

  • Dogan, H.; Dogan, S.D.; Guenduez, M.G.; Krishna, V.S.; Lherbet, C.; Sriram, D.; Sahin, O.; Saripinar, E.
    Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors (2020), Eur. J. Med. Chem., 188, 112035 .
    View publication on PubMed
Search for more literature for 1.3.1.9

Inhibitors

Inhibitors Comment Organism Structure
3-(2-(4-methylbenzylidene)hydrazinyl)-N-(2-(trifluoromethyl)phenyl)-1,2,4-thiadiazol-5-amine 64% inhibition at 0.05 mM, 35% inhibition at 0.005 mM Mycobacterium tuberculosis
3-(2-(4-methylbenzylidene)hydrazinyl)-N-(4-nitrophenyl)-1,2,4-thiadiazol-5-amine 8% inhibition at 0.05 mM Mycobacterium tuberculosis
3-(2-(4-methylbenzylidene)hydrazinyl)-N-(p-tolyl)-1,2,4-thiadiazol-5-amine 21% inhibition at 0.05 mM Mycobacterium tuberculosis
3-(2-(4-methylbenzylidene)hydrazinyl)-N-phenyl-1,2,4-thiadiazol-5-amine 34% inhibition at 0.05 mM Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-(2,4-dichlorophenyl)-1,2,4-thiadiazol-5-amine 38% inhibition at 0.05 mM Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-(2-(trifluoromethyl)phenyl)-1,2,4-thiadiazol-5-amine 50% inhibition at 0.05 mM Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-(4-bromophenyl)-1,2,4-thiadiazol-5-amine 61% inhibition at 0.05 mM, 39% inhibition at 0.005 mM Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-(4-fluorophenyl)-1,2,4-thiadiazol-5-amine 54% inhibition at 0.05 mM Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-(4-iodophenyl)-1,2,4-thiadiazol-5-amine
-
 Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-(4-methoxyphenyl)-1,2,4-thiadiazol-5-amine 46% inhibition at 0.05 mM Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-(4-nitrophenyl)-1,2,4-thiadiazol-5-amine 35% inhibition at 0.05 mM Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-(p-tolyl)-1,2,4-thiadiazol-5-amine 75% inhibition at 0.05 mM, 48% inhibition at 0.005 mM Mycobacterium tuberculosis
3-(2-benzylidenehydrazinyl)-N-phenyl-1,2,4-thiadiazol-5-amine 16% inhibition at 0.05 mM Mycobacterium tuberculosis
cefozopran
-
 Mycobacterium tuberculosis
ciprofloxacine
-
 Mycobacterium tuberculosis
ethambutol
-
 Mycobacterium tuberculosis
isoniazid
-
 Mycobacterium tuberculosis
N-(2,4-dichlorophenyl)-3-(2-(4-methylbenzylidene)hydrazinyl)-1,2,4-thiadiazol-5-amine 62% inhibition at 0.05 mM, 48% inhibition at 0.005 mM Mycobacterium tuberculosis
N-(4-bromophenyl)-3-(2-(4-methylbenzylidene)hydrazinyl)-1,2,4-thiadiazol-5-amine 46% inhibition at 0.05 mM Mycobacterium tuberculosis
N-(4-fluorophenyl)-3-(2-(4-methylbenzylidene)hydrazinyl)-1,2,4-thiadiazol-5-amine 67% inhibition at 0.05 mM, 26% inhibition at 0.005 mM Mycobacterium tuberculosis
N-(4-iodophenyl)-3-(2-(4-methylbenzylidene)hydrazinyl)-1,2,4-thiadiazol-5-amine 34% inhibition at 0.05 mM Mycobacterium tuberculosis
N-(4-methoxyphenyl)-3-(2-(4-methylbenzylidene)hydrazinyl)-1,2,4-thiadiazol-5-amine 50% inhibition at 0.05 mM Mycobacterium tuberculosis
Pyrazinamide
-
 Mycobacterium tuberculosis
rifampicin
-
 Mycobacterium tuberculosis
triclosan more than 99% inhibition at 0.05 mM Mycobacterium tuberculosis

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trans-2-dodecenoyl-CoA + NADH + H+
-
 Mycobacterium tuberculosis dodecanoyl-CoA + NAD+
-
 ?
trans-2-dodecenoyl-CoA + NADH + H+
-
 Mycobacterium tuberculosis H37Rv dodecanoyl-CoA + NAD+
-
 ?

Synonyms

Synonyms Comment Organism
enoyl acyl carrier protein reductase
-
 Mycobacterium tuberculosis
InhA
-
 Mycobacterium tuberculosis

Cofactor

Cofactor Comment Organism Structure
NADH
-
 Mycobacterium tuberculosis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.05
-
 at pH 6.8 and 25°C Mycobacterium tuberculosis 3-(2-benzylidenehydrazinyl)-N-(2-(trifluoromethyl)phenyl)-1,2,4-thiadiazol-5-amine
0.05
-
 at pH 6.8 and 25°C Mycobacterium tuberculosis N-(4-methoxyphenyl)-3-(2-(4-methylbenzylidene)hydrazinyl)-1,2,4-thiadiazol-5-amine