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Literature summary for 3.1.1.8 extracted from

  • Liu, Z.; Fang, L.; Zhang, H.; Gou, S.; Chen, L.
    Design, synthesis and biological evaluation of multifunctional tacrine-curcumin hybrids as new cholinesterase inhibitors with metal ions-chelating and neuroprotective property (2017), Bioorg. Med. Chem., 25, 2387-2398 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
Equus caballus
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
-
Equus caballus
(2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
-
Equus caballus
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
Equus caballus
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
-
Equus caballus
(2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
-
Equus caballus
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
Equus caballus
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
-
Equus caballus
2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide neuroprotective effect of K3-2 against H2O2-induced toxicity Equus caballus
2-(4-hydroxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
Equus caballus
2-(4-hydroxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
-
Equus caballus
2-(4-hydroxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
-
Equus caballus
3-oxo-N-[(1,2,3,4-tetrahydroacridin-9-ylamino)methyl]butanamide
-
Equus caballus
3-oxo-N-[2-(1,2,3,4-tetrahydroacridin-9-ylamino)ethyl]butanamide
-
Equus caballus
3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
-
Equus caballus
3-oxo-N-[5-(1,2,3,4-tetrahydroacridin-9-ylamino)pentyl]butanamide
-
Equus caballus
additional information design, synthesis, and biological evaluation of multifunctional tacrine-curcumin hybrids as cholinesterase inhibitors with metal ions-chelating and neuroprotective properties, overview. The hybrid compounds show good cholinesterase inhibitory activity, some of the compounds exhibit different selectivity on acetylcholinesterase (EC 3.1.1.7) or butyrylcholinesterase due to the structural difference. Structure-activity relationships, molecular modelling, overview Equus caballus
tacrine
-
Equus caballus

Organism

Organism UniProt Comment Textmining
Equus caballus P81908
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Equus caballus
-
serum
-
Equus caballus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
butyrylthiocholine + H2O
-
Equus caballus thiocholine + butyrate
-
?

Synonyms

Synonyms Comment Organism
BChE
-
Equus caballus
butyrylcholinesterase
-
Equus caballus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Equus caballus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
assay at Equus caballus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005
-
pH 8.0, 37°C Equus caballus tacrine
0.00006
-
pH 8.0, 37°C Equus caballus 3-oxo-N-[2-(1,2,3,4-tetrahydroacridin-9-ylamino)ethyl]butanamide
0.00016
-
pH 8.0, 37°C Equus caballus 3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
0.0002
-
pH 8.0, 37°C Equus caballus 2-(4-hydroxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
0.00022
-
pH 8.0, 37°C Equus caballus 2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
0.00022
-
pH 8.0, 37°C Equus caballus 3-oxo-N-[5-(1,2,3,4-tetrahydroacridin-9-ylamino)pentyl]butanamide
0.00031
-
pH 8.0, 37°C Equus caballus 3-oxo-N-[(1,2,3,4-tetrahydroacridin-9-ylamino)methyl]butanamide
0.00039
-
pH 8.0, 37°C Equus caballus 2-(4-hydroxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
0.00083
-
pH 8.0, 37°C Equus caballus 2-(4-hydroxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
0.00131
-
pH 8.0, 37°C Equus caballus 2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
0.0015
-
pH 8.0, 37°C Equus caballus (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
0.0016
-
pH 8.0, 37°C Equus caballus (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
0.00187
-
pH 8.0, 37°C Equus caballus (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide
0.00211
-
pH 8.0, 37°C Equus caballus (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
0.00224
-
pH 8.0, 37°C Equus caballus (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide
0.00338
-
pH 8.0, 37°C Equus caballus 2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide
0.00477
-
pH 8.0, 37°C Equus caballus (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide

General Information

General Information Comment Organism
additional information enzyme homology modeling, molecular modeling, overview Equus caballus