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Literature summary for 3.1.1.7 extracted from
- 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 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | - |
Electrophorus electricus |  |
| (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide | - |
Electrophorus electricus | |
| (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide | - |
Electrophorus electricus | |
| (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | - |
Electrophorus electricus | |
| (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide | - |
Electrophorus electricus | |
| (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide | - |
Electrophorus electricus | |
| 2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | - |
Electrophorus electricus | |
| 2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide | - |
Electrophorus electricus | |
| 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 | Electrophorus electricus | |
| 2-(4-hydroxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | - |
Electrophorus electricus | |
| 2-(4-hydroxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide | - |
Electrophorus electricus | |
| 2-(4-hydroxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide | - |
Electrophorus electricus | |
| 3-oxo-N-[(1,2,3,4-tetrahydroacridin-9-ylamino)methyl]butanamide | - |
Electrophorus electricus | |
| 3-oxo-N-[2-(1,2,3,4-tetrahydroacridin-9-ylamino)ethyl]butanamide | - |
Electrophorus electricus | |
| 3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | - |
Electrophorus electricus | |
| 3-oxo-N-[5-(1,2,3,4-tetrahydroacridin-9-ylamino)pentyl]butanamide | - |
Electrophorus electricus | |
| 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 exhibited different selectivity on acetylcholinesterase or butyrylcholinesterase due to the structural difference. Structure-activity relationships, molecular modelling, overview | Electrophorus electricus | |
| tacrine | - |
Electrophorus electricus | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Electrophorus electricus | O42275 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | - |
Electrophorus electricus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| acetylthiocholine + H2O | - |
Electrophorus electricus | thiocholine + acetate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| AChE | - |
Electrophorus electricus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Electrophorus electricus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
assay at | Electrophorus electricus |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00008 | - |
pH 8.0, 37°C | Electrophorus electricus | 2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide | |
| 0.00009 | - |
pH 8.0, 37°C | Electrophorus electricus | 3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | |
| 0.0001 | - |
pH 8.0, 37°C | Electrophorus electricus | tacrine | |
| 0.00013 | - |
pH 8.0, 37°C | Electrophorus electricus | 2-(4-hydroxybenzyl)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide | |
| 0.00024 | - |
pH 8.0, 37°C | Electrophorus electricus | 3-oxo-N-[2-(1,2,3,4-tetrahydroacridin-9-ylamino)ethyl]butanamide | |
| 0.00029 | - |
pH 8.0, 37°C | Electrophorus electricus | (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide | |
| 0.00046 | - |
pH 8.0, 37°C | Electrophorus electricus | 3-oxo-N-[(1,2,3,4-tetrahydroacridin-9-ylamino)methyl]butanamide | |
| 0.00057 | - |
pH 8.0, 37°C | Electrophorus electricus | 3-oxo-N-[5-(1,2,3,4-tetrahydroacridin-9-ylamino)pentyl]butanamide | |
| 0.00126 | - |
pH 8.0, 37°C | Electrophorus electricus | (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | |
| 0.00199 | - |
pH 8.0, 37°C | Electrophorus electricus | 2-(4-hydroxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide | |
| 0.0021 | - |
pH 8.0, 37°C | Electrophorus electricus | (2E)-2-(4-hydroxy-3-methoxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide | |
| 0.00295 | - |
pH 8.0, 37°C | Electrophorus electricus | (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[6-(1,2,3,4-tetrahydroacridin-9-ylamino)hexyl]butanamide | |
| 0.00368 | - |
pH 8.0, 37°C | Electrophorus electricus | 2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide | |
| 0.0038 | - |
pH 8.0, 37°C | Electrophorus electricus | (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[4-(1,2,3,4-tetrahydroacridin-9-ylamino)butyl]butanamide | |
| 0.00571 | - |
pH 8.0, 37°C | Electrophorus electricus | 2-(4-hydroxy-3-methoxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | |
| 0.00876 | - |
pH 8.0, 37°C | Electrophorus electricus | 2-(4-hydroxybenzyl)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | |
| 0.00964 | - |
pH 8.0, 37°C | Electrophorus electricus | (2E)-2-(4-hydroxybenzylidene)-3-oxo-N-[3-(1,2,3,4-tetrahydroacridin-9-ylamino)propyl]butanamide | |
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