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Literature summary for 3.2.1.18 extracted from

  • Neres, J.; Bonnet, P.; Edwards, P.N.; Kotian, P.L.; Buschiazzo, A.; Alzari, P.M.; Bryce, R.A.; Douglas, K.T.
    Benzoic acid and pyridine derivatives as inhibitors of Trypanosoma cruzi trans-sialidase (2007), Bioorg. Med. Chem., 15, 2106-2119.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
-
Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
3-(2-amino-1-hydroxyethyl)-4-[(methylsulfonyl)amino]benzoic acid 1 mM, 17% inhibition Trypanosoma cruzi
3-(acetylamino)-4-morpholin-4-ylbenzoic acid
-
Trypanosoma cruzi
3-amino-4-(benzylthio)benzoic acid
-
Trypanosoma cruzi
3-amino-4-(pyridin-3-ylamino)benzoic acid
-
Trypanosoma cruzi
3-amino-4-[(phenylacetyl)amino]benzoic acid
-
Trypanosoma cruzi
3-[(aminoacetyl)amino]-4-(benzylthio)benzoic acid
-
Trypanosoma cruzi
3-[(diaminomethylene)amino]-4-[(methylamino)carbonyl]benzoic acid
-
Trypanosoma cruzi
3-[(diaminomethylene)amino]-4-[(methylsulfinyl)amino]benzoic acid 1 mM, 29% inhibition Trypanosoma cruzi
3-[(diaminomethylene)amino]-4-[(phenylacetyl)amino]benzoic acid 1 mM, 54% inhibition Trypanosoma cruzi
3-[(diaminomethylene)amino]-5-(hydroxymethyl)-4-[(methylsulfonyl)amino]benzoic acid 1 mM, 11% inhibition Trypanosoma cruzi
3-[(diaminomethylene)amino]-5-[(E)-(hydroxyimino)methyl]-4-[(methylsulfonyl)amino]benzoic acid 1 mM, 46% inhibition Trypanosoma cruzi
3-[(diaminomethylene)amino]-5-[(E)-(hydroxyimino)methyl]benzoic acid 1 mM, 35% inhibition Trypanosoma cruzi
4-(acetylamino)-3-(2,3-dihydroxypropyl)benzoic acid 1 mM, 17% inhibition Trypanosoma cruzi
4-(acetylamino)-3-(2-aminoethyl)benzoic acid 1 mM, 25% inhibition Trypanosoma cruzi
4-(acetylamino)-3-(2-hydroxyethyl)benzoic acid 1 mM, 16% inhibition Trypanosoma cruzi
4-(acetylamino)-3-(hydroxymethyl)benzoic acid
-
Trypanosoma cruzi
4-(acetylamino)-3-[(diaminomethylene)amino]benzoic acid 1 mM, 41% inhibition Trypanosoma cruzi
4-(acetylamino)-3-[(Z)-(hydroxyimino)methyl]benzoic acid 1 mM, 24% inhibition Trypanosoma cruzi
4-(benzylamino)-3-[(diaminomethylene)amino]benzoic acid 1 mM, 9% inhibition Trypanosoma cruzi
4-(benzylthio)-3-[(diaminomethylene)amino]benzoic acid 1 mM, 43% inhibition Trypanosoma cruzi
5-(acetylamino)-4-aminopyridine-2-carboxylic acid 1 mM, 14% inhibition Trypanosoma cruzi
5-(acetylamino)-6-aminopyridine-2-carboxylic acid
-
Trypanosoma cruzi
5-(acetylamino)pyridine-2-carboxylic acid 1 mM, 22% inhibition Trypanosoma cruzi
5-(ethanethioylamino)pyridine-2-carboxylic acid
-
Trypanosoma cruzi
5-[(methylsulfonyl)amino]pyridine-2-carboxylic acid 1 mM, 25% inhibition Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Trypanosoma cruzi

Synonyms

Synonyms Comment Organism
TcTS
-
Trypanosoma cruzi
trans-sialidase
-
Trypanosoma cruzi

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.44
-
-
Trypanosoma cruzi 5-(acetylamino)-6-aminopyridine-2-carboxylic acid
0.54
-
-
Trypanosoma cruzi 4-(acetylamino)-3-(hydroxymethyl)benzoic acid
0.54
-
-
Trypanosoma cruzi 5-(ethanethioylamino)pyridine-2-carboxylic acid
0.58
-
-
Trypanosoma cruzi 3-(acetylamino)-4-morpholin-4-ylbenzoic acid
0.7
-
-
Trypanosoma cruzi 3-amino-4-(benzylthio)benzoic acid
0.74
-
-
Trypanosoma cruzi 3-amino-4-(pyridin-3-ylamino)benzoic acid
0.76
-
-
Trypanosoma cruzi 3-[(diaminomethylene)amino]-4-[(methylamino)carbonyl]benzoic acid
1
-
-
Trypanosoma cruzi 3-[(aminoacetyl)amino]-4-(benzylthio)benzoic acid
1.2
-
-
Trypanosoma cruzi 3-amino-4-[(phenylacetyl)amino]benzoic acid