Page last updated: 2024-08-07 15:41:30
Cholinesterase
A cholinesterase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P06276]
Synonyms
EC 3.1.1.8;
Acylcholine acylhydrolase;
Butyrylcholine esterase;
Choline esterase II;
Pseudocholinesterase
Research
Bioassay Publications (276)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (0.36) | 18.7374 |
| 1990's | 9 (3.26) | 18.2507 |
| 2000's | 64 (23.19) | 29.6817 |
| 2010's | 150 (54.35) | 24.3611 |
| 2020's | 52 (18.84) | 2.80 |
Compounds (174)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| diacetyl | Homo sapiens (human) | Ki | 100.0000 | 3 | 8 |
| thioctic acid | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 2 |
| melatonin | Homo sapiens (human) | IC50 | 0.1000 | 1 | 2 |
| xanthine | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| huperzine a | Homo sapiens (human) | IC50 | 4.4288 | 4 | 7 |
| huperzine a | Homo sapiens (human) | Ki | 0.5235 | 1 | 2 |
| bw 284 c 51 | Homo sapiens (human) | IC50 | 24.0090 | 1 | 2 |
| 6,7-dichloroquinoxaline-2,3-dione | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| 6-methoxytryptoline | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| oxyquinoline | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| tacrine | Homo sapiens (human) | IC50 | 0.0545 | 115 | 132 |
| tacrine | Homo sapiens (human) | Ki | 0.0417 | 7 | 8 |
| benextramine | Homo sapiens (human) | IC50 | 6.1659 | 2 | 2 |
| berberine | Homo sapiens (human) | IC50 | 15.8950 | 2 | 2 |
| caffeine | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| chelerythrine | Homo sapiens (human) | IC50 | 8.5800 | 1 | 1 |
| benzophenone | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| donepezil | Homo sapiens (human) | IC50 | 5.4658 | 81 | 85 |
| donepezil | Homo sapiens (human) | Ki | 4.7266 | 3 | 4 |
| edrophonium | Homo sapiens (human) | Ki | 99.5050 | 1 | 2 |
| profenamine | Homo sapiens (human) | IC50 | 0.2550 | 2 | 2 |
| profenamine | Homo sapiens (human) | Ki | 0.0200 | 2 | 2 |
| huprine x | Homo sapiens (human) | Ki | 0.0600 | 1 | 2 |
| ibuprofen | Homo sapiens (human) | IC50 | 600.0000 | 1 | 1 |
| methoctramine | Homo sapiens (human) | IC50 | 0.9772 | 2 | 2 |
| clorgyline | Homo sapiens (human) | IC50 | 500.0000 | 1 | 1 |
| neostigmine | Homo sapiens (human) | IC50 | 18.4800 | 4 | 5 |
| neostigmine | Homo sapiens (human) | Ki | 35.5000 | 1 | 2 |
| quinone | Homo sapiens (human) | Ki | 57.8650 | 2 | 7 |
| pentoxifylline | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| 1,3a,8-Trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl methylcarbamate | Homo sapiens (human) | IC50 | 0.0194 | 4 | 8 |
| propentofylline | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| propidium | Homo sapiens (human) | IC50 | 17.2630 | 1 | 3 |
| propidium | Homo sapiens (human) | Ki | 4.0633 | 2 | 3 |
| pyridostigmine | Homo sapiens (human) | IC50 | 8,020.0000 | 1 | 2 |
| pyridostigmine | Homo sapiens (human) | Ki | 3.5000 | 1 | 1 |
| saccharin | Homo sapiens (human) | IC50 | 3.6000 | 1 | 1 |
| sanguinarine | Homo sapiens (human) | IC50 | 7.0800 | 1 | 1 |
| sulfanilamide | Homo sapiens (human) | IC50 | 138.7900 | 1 | 1 |
| tetraisopropylpyrophosphamide | Homo sapiens (human) | IC50 | 113.7047 | 2 | 3 |
| donepezil hydrochloride | Homo sapiens (human) | IC50 | 7.1830 | 2 | 3 |
| physostigmine | Homo sapiens (human) | IC50 | 1,455,053,333,334.3850 | 25 | 30 |
| physostigmine | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| veratramine | Homo sapiens (human) | IC50 | 19.4600 | 1 | 1 |
| berlition | Homo sapiens (human) | IC50 | 1,000.0000 | 2 | 2 |
| androstenedione | Homo sapiens (human) | IC50 | 1.5500 | 1 | 1 |
| acenaphthenequinone | Homo sapiens (human) | Ki | 21.2282 | 3 | 5 |
| 9,10-phenanthrenequinone | Homo sapiens (human) | Ki | 20.0869 | 3 | 5 |
| 5-bromoisatin | Homo sapiens (human) | Ki | 51.3743 | 2 | 7 |
| isatin | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| chloranil | Homo sapiens (human) | Ki | 0.1492 | 2 | 6 |
| benzoin | Homo sapiens (human) | Ki | 72.7814 | 3 | 7 |
| dibenzoylmethane | Homo sapiens (human) | Ki | 71.6583 | 2 | 6 |
| benzil | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| benzil | Homo sapiens (human) | Ki | 61.5635 | 7 | 13 |
| paraoxon | Homo sapiens (human) | IC50 | 0.0070 | 1 | 1 |
| galantamine | Homo sapiens (human) | IC50 | 681.1987 | 38 | 42 |
| galantamine | Homo sapiens (human) | Ki | 9.5583 | 3 | 3 |
| benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(n,n-dimethyl-n-2-propenyl-), dibromide | Homo sapiens (human) | IC50 | 354.0000 | 1 | 1 |
| benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(n,n-dimethyl-n-2-propenyl-), dibromide | Homo sapiens (human) | Ki | 0.0500 | 1 | 1 |
| rhein | Homo sapiens (human) | IC50 | 17.0000 | 1 | 1 |
| vasicinone | Homo sapiens (human) | IC50 | 10.2000 | 1 | 1 |
| 1,3-cyclohexanedione | Homo sapiens (human) | Ki | 100.0000 | 2 | 7 |
| dibromsalicil | Homo sapiens (human) | Ki | 66.6877 | 2 | 6 |
| 1,2-naphthoquinone | Homo sapiens (human) | Ki | 1.6460 | 3 | 5 |
| jkl 1073a | Homo sapiens (human) | IC50 | 68.0000 | 1 | 1 |
| 1-acetylisatin | Homo sapiens (human) | Ki | 89.3333 | 2 | 6 |
| 1-phenyl-1,2-propanedione | Homo sapiens (human) | Ki | 58.8629 | 3 | 7 |
| 2,3-pentanedione | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| 5-methylisatin | Homo sapiens (human) | Ki | 87.7000 | 2 | 6 |
| Berberine chloride (TN) | Homo sapiens (human) | IC50 | 33.0850 | 2 | 2 |
| 1,2-cyclohexanedione | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| boldenone | Homo sapiens (human) | IC50 | 20.8700 | 1 | 1 |
| vinblastine | Homo sapiens (human) | IC50 | 2.1000 | 1 | 1 |
| 1,4-androstadiene-3,17-dione | Homo sapiens (human) | IC50 | 102.6600 | 1 | 1 |
| n-methylisatin | Homo sapiens (human) | Ki | 73.9300 | 2 | 6 |
| thioflavin t | Homo sapiens (human) | Ki | 0.8000 | 1 | 1 |
| thioflavin t | Homo sapiens (human) | Ki | 4.3050 | 1 | 2 |
| palmatine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| selegiline | Homo sapiens (human) | IC50 | 250.0028 | 2 | 2 |
| acetylacetone | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| 5-Methoxyisatin | Homo sapiens (human) | Ki | 87.7833 | 2 | 6 |
| bambuterol | Homo sapiens (human) | IC50 | 0.0033 | 4 | 4 |
| 3-methyl-1,2-cyclopentanedione | Homo sapiens (human) | Ki | 85.9500 | 2 | 6 |
| pralidoxime iodide | Homo sapiens (human) | Ki | 390.0000 | 1 | 1 |
| geneserine | Homo sapiens (human) | IC50 | 0.0810 | 1 | 2 |
| physostigmine heptyl | Homo sapiens (human) | IC50 | 0.0135 | 1 | 2 |
| 2,3-trimethylene-4-quinazolone | Homo sapiens (human) | IC50 | 29.3400 | 3 | 3 |
| 4-benzoylbenzoic acid | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| adrenoglomerulotropin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| chelerythrine chloride | Homo sapiens (human) | IC50 | 10.3400 | 1 | 1 |
| 1,10-phenanthroline-5,6-dione | Homo sapiens (human) | Ki | 81.0800 | 3 | 5 |
| 1,2,3,6-tetragalloylglucose | Homo sapiens (human) | IC50 | 18.2900 | 1 | 1 |
| 2-chloranil | Homo sapiens (human) | Ki | 2.5700 | 2 | 6 |
| 3,5-di-tert-butyl-1,2-benzoquinone | Homo sapiens (human) | Ki | 50.3624 | 2 | 6 |
| rivastigmine | Homo sapiens (human) | IC50 | 2.7549 | 39 | 42 |
| 5-Chloro-1H-indole-2,3-dione | Homo sapiens (human) | Ki | 53.4150 | 2 | 6 |
| 5-iodoisatin | Homo sapiens (human) | Ki | 58.4767 | 2 | 6 |
| 2,2-dimethoxy-2-phenylacetophenone | Homo sapiens (human) | Ki | 85.8833 | 2 | 6 |
| anisoin | Homo sapiens (human) | Ki | 85.6500 | 2 | 6 |
| hydrobenzoin | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| propidium iodide | Homo sapiens (human) | IC50 | 13.2000 | 6 | 6 |
| methoctramine | Homo sapiens (human) | IC50 | 0.9772 | 1 | 1 |
| 7-methoxytacrine | Homo sapiens (human) | IC50 | 16.6120 | 5 | 5 |
| razadyne | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| profenamine hydrochloride | Homo sapiens (human) | IC50 | 1.6000 | 1 | 1 |
| profenamine hydrochloride | Homo sapiens (human) | Ki | 12,100.0000 | 1 | 1 |
| 1,3-indandione | Homo sapiens (human) | Ki | 23.1940 | 3 | 5 |
| safinamide | Homo sapiens (human) | IC50 | 0.0052 | 1 | 2 |
| safinamide | Homo sapiens (human) | Ki | 0.0023 | 1 | 1 |
| barbigerone | Homo sapiens (human) | IC50 | 21.7700 | 1 | 1 |
| testololactone | Homo sapiens (human) | IC50 | 142.4500 | 1 | 1 |
| chonemorphine | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| sch 58261 | Homo sapiens (human) | Ki | 5.0006 | 2 | 4 |
| dizocilpine | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| phenserine | Homo sapiens (human) | IC50 | 1.0477 | 4 | 6 |
| latrepirdine | Homo sapiens (human) | IC50 | 3,953.9500 | 2 | 2 |
| 5-Fluoroisatin | Homo sapiens (human) | Ki | 100.0000 | 2 | 7 |
| berbamine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| N-butyl-1H-benzimidazol-2-amine | Homo sapiens (human) | IC50 | 61.0100 | 1 | 1 |
| aromoline | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| aromoline | Homo sapiens (human) | Ki | 23.0550 | 2 | 2 |
| obamegine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| quinidine | Homo sapiens (human) | IC50 | 1.2300 | 1 | 1 |
| hemanthamine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| physovenine | Homo sapiens (human) | IC50 | 0.0067 | 1 | 1 |
| 3-deoxyvasicine | Homo sapiens (human) | IC50 | 0.0400 | 1 | 1 |
| resveratrol | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| ferulic acid | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| cyclosaligenyl-2',3'-didehydro-2',3'-dideoxythymidine monophosphate | Homo sapiens (human) | IC50 | 0.7700 | 2 | 2 |
| ganoderiol f | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| chalcone | Homo sapiens (human) | IC50 | 87.0000 | 1 | 1 |
| 2'-hydroxychalcone | Homo sapiens (human) | IC50 | 84.0000 | 1 | 1 |
| 2,2'-dihydroxychalcone | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| vasicine | Homo sapiens (human) | IC50 | 3.1300 | 1 | 1 |
| 4-amino-5-(pyridin-4-yl)-4h-1,2,4-triazole-3-thiol | Homo sapiens (human) | IC50 | 49.5800 | 1 | 1 |
| huperzine a | Homo sapiens (human) | IC50 | 5,050.0000 | 2 | 2 |
| curcumin | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| 1-[(3,4-dichlorophenyl)methyl]indole-2,3-dione | Homo sapiens (human) | Ki | 12.2605 | 2 | 6 |
| tacrine hydrochloride | Homo sapiens (human) | IC50 | 0.0430 | 4 | 4 |
| k 858 | Homo sapiens (human) | IC50 | 0.0049 | 1 | 1 |
| Ganodermanontriol | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| hirsutine | Homo sapiens (human) | IC50 | 1.9700 | 1 | 1 |
| azilect | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| rasagiline | Homo sapiens (human) | IC50 | 2.3865 | 2 | 2 |
| 5-Nitroisatin | Homo sapiens (human) | Ki | 84.4050 | 2 | 6 |
| trans-2,3',4,5'-tetrahydroxystilbene | Homo sapiens (human) | IC50 | 2.9500 | 1 | 1 |
| 4'-hydroxychalcone | Homo sapiens (human) | IC50 | 500.0000 | 1 | 1 |
| mre 3008-f20 | Homo sapiens (human) | Ki | 0.0707 | 2 | 8 |
| vinorelbine | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| catharanthine | Homo sapiens (human) | IC50 | 3.1700 | 1 | 1 |
| 4-hydroxylonchocarpin | Homo sapiens (human) | IC50 | 4.1250 | 2 | 2 |
| 4-hydroxylonchocarpin | Homo sapiens (human) | Ki | 3.4800 | 1 | 1 |
| ciproxifan | Homo sapiens (human) | IC50 | 77.3000 | 2 | 2 |
| ith 4012 | Homo sapiens (human) | IC50 | 5.0000 | 2 | 2 |
| bis(7)-tacrine | Homo sapiens (human) | IC50 | 0.0142 | 4 | 5 |
| bis(7)-tacrine | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| phenethylcymserine | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| ganstigmine | Homo sapiens (human) | IC50 | 0.1875 | 1 | 2 |
| ap 2238 | Homo sapiens (human) | IC50 | 48.9000 | 5 | 6 |
| ap 2238 | Homo sapiens (human) | Ki | 0.0217 | 1 | 1 |
| cymserine | Homo sapiens (human) | IC50 | 0.2529 | 5 | 7 |
| memoquin | Homo sapiens (human) | IC50 | 1.1808 | 5 | 5 |
| tolserine | Homo sapiens (human) | IC50 | 1.1740 | 3 | 5 |
| pf9601n | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| caproctamine | Homo sapiens (human) | IC50 | 14,185,633,343.0745 | 6 | 6 |
| huprine y | Homo sapiens (human) | IC50 | 0.1762 | 5 | 8 |
| arisugacin | Homo sapiens (human) | IC50 | 18.0000 | 1 | 1 |
| 6-chlorotacrine | Homo sapiens (human) | IC50 | 0.8458 | 10 | 12 |
| 9-hydroxy-4-androstene-3,17-dione | Homo sapiens (human) | IC50 | 141.2800 | 1 | 1 |
| 4-Methoxylonchocarpin | Homo sapiens (human) | IC50 | 101.9100 | 1 | 1 |
| xanthostigmine | Homo sapiens (human) | IC50 | 6.8847 | 5 | 7 |
| montanine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| mb 05032 | Homo sapiens (human) | IC50 | 0.0160 | 1 | 2 |
| lipocrine | Homo sapiens (human) | IC50 | 0.0109 | 4 | 4 |
| lipocrine | Homo sapiens (human) | Ki | 0.1550 | 1 | 1 |
| adl 5859 | Homo sapiens (human) | IC50 | 78.0000 | 1 | 1 |
| ganodermadiol | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| lucidenic acid a | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| lucidenic acid n | Homo sapiens (human) | IC50 | 188.3600 | 1 | 1 |
| olaparib | Homo sapiens (human) | IC50 | 0.0035 | 2 | 2 |
| ass234 | Homo sapiens (human) | IC50 | 2.0920 | 5 | 5 |
| dicumarol | Homo sapiens (human) | IC50 | 0.0026 | 1 | 1 |
| ganoderic acid y | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| pralidoxime | Homo sapiens (human) | IC50 | 878.0000 | 1 | 1 |
| asoxime chloride | Homo sapiens (human) | Ki | 215.0000 | 1 | 1 |
| obidoxime chloride | Homo sapiens (human) | IC50 | 1,910.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| dapagliflozin | Homo sapiens (human) | EC50 | 0.0024 | 1 | 1 |
Drugs with Other Measurements
Requirements for mammalian carboxylesterase inhibition by substituted ethane-1,2-diones.Bioorganic & medicinal chemistry, , Aug-01, Volume: 19, Issue:15, 2011
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Design, synthesis and biological evaluation of coumarin derivatives as novel acetylcholinesterase inhibitors that attenuate H2O2-induced apoptosis in SH-SY5Y cells.Bioorganic chemistry, , Volume: 68, 2016
Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
[no title available]Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 61, 2022
Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents.European journal of medicinal chemistry, , Mar-05, Volume: 231, 2022
Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model.RSC medicinal chemistry, , Aug-17, Volume: 13, Issue:8, 2022
[no title available]RSC medicinal chemistry, , Jul-20, Volume: 13, Issue:7, 2022
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
[no title available]Journal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 43, 2021
Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters.European journal of medicinal chemistry, , Jun-05, Volume: 218, 2021
Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HTEuropean journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HTEuropean journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
Rapid discovery of a selective butyrylcholinesterase inhibitor using structure-based virtual screening.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 30, Issue:24, 2020
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6.Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Discovery of potent and selective butyrylcholinesterase inhibitors through the use of pharmacophore-based screening.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo.Journal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Synthesis and evaluation of tetrahydroisoquinoline-benzimidazole hybrids as multifunctional agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
Tacrines for Alzheimer's disease therapy. III. The PyridoTacrines.European journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
Alkaloids from the Branches and Leaves of Journal of natural products, , 12-27, Volume: 82, Issue:12, 2019
Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids.European journal of medicinal chemistry, , Mar-25, Volume: 148, 2018
Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Tacripyrimidines, the first tacrine-dihydropyrimidine hybrids, as multi-target-directed ligands for Alzheimer's disease.European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
[no title available]Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
[no title available]ACS medicinal chemistry letters, , Mar-08, Volume: 9, Issue:3, 2018
New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents.Bioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.European journal of medicinal chemistry, , Apr-21, Volume: 130, 2017
5-Methyl-MedChemComm, , Jun-01, Volume: 8, Issue:6, 2017
Novel deoxyvasicinone derivatives as potent multitarget-directed ligands for the treatment of Alzheimer's disease: Design, synthesis, and biological evaluation.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
New tacrine-derived AChE/BuChE inhibitors: Synthesis and biological evaluation of 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates.European journal of medicinal chemistry, , Mar-10, Volume: 128, 2017
Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease.Chemical biology & drug design, , Volume: 88, Issue:5, 2016
Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography.Journal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators.Journal of medicinal chemistry, , 11-10, Volume: 59, Issue:21, 2016
Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Iminosugars as a new class of cholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 25, Issue:4, 2015
Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.European journal of medicinal chemistry, , May-05, Volume: 95, 2015
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.Journal of medicinal chemistry, , Aug-28, Volume: 57, Issue:16, 2014
Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
Synthesis, biological evaluation and molecular modeling of substituted 2-aminobenzimidazoles as novel inhibitors of acetylcholinesterase and butyrylcholinesterase.Bioorganic & medicinal chemistry, , Jul-15, Volume: 21, Issue:14, 2013
Selective inhibition of human acetylcholinesterase by xanthine derivatives: in vitro inhibition and molecular modeling investigations.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.Bioorganic & medicinal chemistry, , Jan-01, Volume: 21, Issue:1, 2013
Quinones bearing non-steroidal anti-inflammatory fragments as multitarget ligands for Alzheimer's disease.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 54, 2012
Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine.European journal of medicinal chemistry, , Volume: 52, 2012
New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties.Journal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase.Bioorganic & medicinal chemistry, , Nov-15, Volume: 20, Issue:22, 2012
Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
(+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's diJournal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:8, 2011
New potent human acetylcholinesterase inhibitors in the tetracyclic triterpene series with inhibitory potency on amyloid β aggregation.European journal of medicinal chemistry, , Volume: 46, Issue:6, 2011
Homodimeric bis-quaternary heterocyclic ammonium salts as potent acetyl- and butyrylcholinesterase inhibitors: a systematic investigation of the influence of linker and cationic heads over affinity and selectivity.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 18, Issue:19, 2008
Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics.Bioorganic & medicinal chemistry, , Oct-15, Volume: 15, Issue:20, 2007
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the oxyanion hole.Journal of medicinal chemistry, , Nov-16, Volume: 49, Issue:23, 2006
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Donepezil-tacrine hybrid related derivatives as new dual binding site inhibitors of AChE.Bioorganic & medicinal chemistry, , Dec-15, Volume: 13, Issue:24, 2005
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Rational approach to discover multipotent anti-Alzheimer drugs.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.Journal of medicinal chemistry, , Dec-16, Volume: 47, Issue:26, 2004
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Homodimeric tacrine congeners as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Acetylcholinesterase inhibitors for potential use in Alzheimer's disease: molecular modeling, synthesis and kinetic evaluation of 11H-indeno-[1,2-b]-quinolin-10-ylamine derivatives.Bioorganic & medicinal chemistry, , Volume: 8, Issue:3, 2000
Aminopyridazines as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety.Journal of medicinal chemistry, , Jul-21, Volume: 38, Issue:15, 1995
Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Mar-31, Volume: 38, Issue:7, 1995
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.Journal of medicinal chemistry, , Aug-21, Volume: 35, Issue:17, 1992
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.Journal of natural products, , 02-22, Volume: 82, Issue:2, 2019
Isolation of cholinesterase and β-secretase 1 inhibiting compounds from Lycopodiella cernua.Bioorganic & medicinal chemistry, , Jul-01, Volume: 23, Issue:13, 2015
Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 61, 2022
Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents.European journal of medicinal chemistry, , Mar-05, Volume: 231, 2022
Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
[no title available]RSC medicinal chemistry, , Jul-20, Volume: 13, Issue:7, 2022
Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Discovery of new phenyl sulfonyl-pyrimidine carboxylate derivatives as the potential multi-target drugs with effective anti-Alzheimer's action: Design, synthesis, crystal structure and in-vitro biological evaluation.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease.European journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-15, Volume: 192, 2020
Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease.Bioorganic & medicinal chemistry, , 11-15, Volume: 28, Issue:22, 2020
Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Design, synthesis and biological evaluation of 2,3-dihydro-5,6-dimethoxy-1H-inden-1-one and piperazinium salt hybrid derivatives as hAChE and hBuChE enzyme inhibitors.European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Highly potent and selective aryl-1,2,3-triazolyl benzylpiperidine inhibitors toward butyrylcholinesterase in Alzheimer's disease.Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Design and development of molecular hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles as potential multifunctional agents to treat Alzheimer's disease.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Investigating 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole as scaffold of butyrylcholinesterase-selective inhibitors with additional neuroprotective activities for Alzheimer's disease.European journal of medicinal chemistry, , Sep-01, Volume: 177, 2019
Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease.Bioorganic & medicinal chemistry, , 08-15, Volume: 27, Issue:16, 2019
Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties.European journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.European journal of medicinal chemistry, , Apr-21, Volume: 130, 2017
Synthesis and pharmacological evaluation of multi-functional homoisoflavonoid derivatives as potent inhibitors of monoamine oxidase B and cholinesterase for the treatment of Alzheimer's disease.MedChemComm, , Jul-01, Volume: 8, Issue:7, 2017
Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 27, Issue:22, 2017
From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Enzymatic and solid-phase synthesis of new donepezil-based L- and d-glutamic acid derivatives and their pharmacological evaluation in models related to Alzheimer's disease and cerebral ischemia.European journal of medicinal chemistry, , Apr-21, Volume: 130, 2017
Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-21, Volume: 130, 2017
Synthesis, structure-activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease.Chemical biology & drug design, , Volume: 88, Issue:5, 2016
Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin.Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
New cinnamic - N-benzylpiperidine and cinnamic - N,N-dibenzyl(N-methyl)amine hybrids as Alzheimer-directed multitarget drugs with antioxidant, cholinergic, neuroprotective and neurogenic properties.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
New multifunctional melatonin-derived benzylpyridinium bromides with potent cholinergic, antioxidant, and neuroprotective properties as innovative drugs for Alzheimer's disease.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.Journal of medicinal chemistry, , Dec-26, Volume: 57, Issue:24, 2014
Synthesis, crystal structure and biological evaluation of some novel 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Active compounds from a diverse library of triazolothiadiazole and triazolothiadiazine scaffolds: synthesis, crystal structure determination, cytotoxicity, cholinesterase inhibitory activity, and binding mode analysis.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Synthesis, cytotoxicity and molecular modelling studies of new phenylcinnamide derivatives as potent inhibitors of cholinesterases.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Synthesis of α, β-unsaturated carbonyl based compounds as acetylcholinesterase and butyrylcholinesterase inhibitors: characterization, molecular modeling, QSAR studies and effect against amyloid β-induced cytotoxicity.European journal of medicinal chemistry, , Aug-18, Volume: 83, 2014
Selective inhibition of human acetylcholinesterase by xanthine derivatives: in vitro inhibition and molecular modeling investigations.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Design, synthesis and evaluation of some new 4-aminopyridine derivatives in learning and memory.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.Bioorganic & medicinal chemistry, , Jan-01, Volume: 21, Issue:1, 2013
Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: synthesis, biological assessment, and molecular modeling.European journal of medicinal chemistry, , Volume: 57, 2012
Synthesis and biological evaluation of 3-thiazolocoumarinyl Schiff-base derivatives as cholinesterase inhibitors.Chemical biology & drug design, , Volume: 80, Issue:4, 2012
(+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
Homodimeric bis-quaternary heterocyclic ammonium salts as potent acetyl- and butyrylcholinesterase inhibitors: a systematic investigation of the influence of linker and cationic heads over affinity and selectivity.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011
Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:3, 2009
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics.Bioorganic & medicinal chemistry, , Oct-15, Volume: 15, Issue:20, 2007
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Donepezil-tacrine hybrid related derivatives as new dual binding site inhibitors of AChE.Bioorganic & medicinal chemistry, , Dec-15, Volume: 13, Issue:24, 2005
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.Journal of medicinal chemistry, , Dec-16, Volume: 47, Issue:26, 2004
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Aminopyridazines as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Mar-31, Volume: 38, Issue:7, 1995
[no title available]Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Discovery of potent and selective butyrylcholinesterase inhibitors through the use of pharmacophore-based screening.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors.Journal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Synthesis, crystal structure and biological evaluation of some novel 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Active compounds from a diverse library of triazolothiadiazole and triazolothiadiazine scaffolds: synthesis, crystal structure determination, cytotoxicity, cholinesterase inhibitory activity, and binding mode analysis.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Synthesis, cytotoxicity and molecular modelling studies of new phenylcinnamide derivatives as potent inhibitors of cholinesterases.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Synthesis and biological evaluation of 3-thiazolocoumarinyl Schiff-base derivatives as cholinesterase inhibitors.Chemical biology & drug design, , Volume: 80, Issue:4, 2012
The preparation, in vitro screening and molecular docking of symmetrical bisquaternary cholinesterase inhibitors containing a but-(2E)-en-1,4-diyl connecting linkage.Journal of enzyme inhibition and medicinal chemistry, , Volume: 26, Issue:2, 2011
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
[no title available]Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Probing the peripheral site of human butyrylcholinesterase.Biochemistry, , Sep-11, Volume: 51, Issue:36, 2012
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.Journal of medicinal chemistry, , Sep-10, Volume: 52, Issue:17, 2009
The preparation, in vitro screening and molecular docking of symmetrical bisquaternary cholinesterase inhibitors containing a but-(2E)-en-1,4-diyl connecting linkage.Journal of enzyme inhibition and medicinal chemistry, , Volume: 26, Issue:2, 2011
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.Journal of medicinal chemistry, , Volume: 32, Issue:7, 1989
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 51, 2021
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.Journal of natural products, , 05-22, Volume: 83, Issue:5, 2020
Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.Bioorganic chemistry, , Volume: 64, 2016
Synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory potential of hydrazide based Schiff bases.Bioorganic chemistry, , Volume: 68, 2016
Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase.Bioorganic chemistry, , Volume: 63, 2015
Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Dual inhibition of the α-glucosidase and butyrylcholinesterase studied by molecular field topology analysis.European journal of medicinal chemistry, , Jun-10, Volume: 80, 2014
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.Journal of medicinal chemistry, , Dec-16, Volume: 47, Issue:26, 2004
New triterpenoid alkaloid cholinesterase inhibitors from Buxus hyrcana.Journal of natural products, , Volume: 66, Issue:6, 2003
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Jan-04, Volume: 44, Issue:1, 2001
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.Journal of medicinal chemistry, , Aug-29, Volume: 40, Issue:18, 1997
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety.Journal of medicinal chemistry, , Jul-21, Volume: 38, Issue:15, 1995
Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Mar-31, Volume: 38, Issue:7, 1995
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.Journal of medicinal chemistry, , Aug-21, Volume: 35, Issue:17, 1992
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.Journal of medicinal chemistry, , Volume: 32, Issue:7, 1989
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.Bioorganic & medicinal chemistry, , Jun-01, Volume: 15, Issue:11, 2007
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
Requirements for mammalian carboxylesterase inhibition by substituted ethane-1,2-diones.Bioorganic & medicinal chemistry, , Aug-01, Volume: 19, Issue:15, 2011
Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.Bioorganic & medicinal chemistry, , Jun-01, Volume: 15, Issue:11, 2007
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 51, 2021
"Clicking" fragment leads to novel dual-binding cholinesterase inhibitors.Bioorganic & medicinal chemistry, , 07-15, Volume: 42, 2021
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.Journal of natural products, , 05-22, Volume: 83, Issue:5, 2020
Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
Design, synthesis and biological evaluation of 2,3-dihydro-5,6-dimethoxy-1H-inden-1-one and piperazinium salt hybrid derivatives as hAChE and hBuChE enzyme inhibitors.European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Design, synthesis and cholinesterase inhibitory activity of novel spiropyrrolidine tethered imidazole heterocyclic hybrids.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.Journal of natural products, , 02-22, Volume: 82, Issue:2, 2019
Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 29, Issue:10, 2019
Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
A Bioactive Resveratrol Trimer from the Stem Bark of the Sri Lankan Endemic Plant Vateria copallifera.Journal of natural products, , 08-24, Volume: 81, Issue:8, 2018
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
2-Arylbenzofurans from Artocarpus lakoocha and methyl ether analogs with potent cholinesterase inhibitory activity.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Green synthesis of novel spiro-indenoquinoxaline derivatives and their cholinesterases inhibition activity.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 27, Issue:2, 2017
Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease.Chemical biology & drug design, , Volume: 88, Issue:5, 2016
Cholinesterase inhibitory activity of isoquinoline alkaloids from three Cryptocarya species (Lauraceae).Bioorganic & medicinal chemistry, , 09-15, Volume: 24, Issue:18, 2016
Coumarin hybrids as novel therapeutic agents.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 2014
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.Bioorganic & medicinal chemistry, , Jan-01, Volume: 21, Issue:1, 2013
Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease.Bioorganic & medicinal chemistry letters, , May-01, Volume: 23, Issue:9, 2013
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase.Bioorganic & medicinal chemistry, , Nov-15, Volume: 20, Issue:22, 2012
(+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
Antioxidant and anticholinesterase activity evaluation of ent-kaurane diterpenoids from Sideritis arguta.Journal of natural products, , Mar-27, Volume: 72, Issue:3, 2009
Butyrylcholinesterase inhibitory activity of testosterone and some of its metabolites.Journal of enzyme inhibition and medicinal chemistry, , Volume: 24, Issue:2, 2009
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Bioactive 5alpha-pregnane-type steroidal alkaloids from Sarcococca hookeriana.Journal of natural products, , Volume: 71, Issue:8, 2008
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.Journal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Requirements for mammalian carboxylesterase inhibition by substituted ethane-1,2-diones.Bioorganic & medicinal chemistry, , Aug-01, Volume: 19, Issue:15, 2011
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 61, 2022
Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease.European journal of medicinal chemistry, , May-26, Volume: 132, 2017
Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Therapeutic potential of quinazoline derivatives for Alzheimer's disease: A comprehensive review.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Novel deoxyvasicinone derivatives as potent multitarget-directed ligands for the treatment of Alzheimer's disease: Design, synthesis, and biological evaluation.European journal of medicinal chemistry, , Nov-10, Volume: 140, 2017
Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents.European journal of medicinal chemistry, , Mar-05, Volume: 231, 2022
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model.RSC medicinal chemistry, , Aug-17, Volume: 13, Issue:8, 2022
Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Design and synthesis of garlic-related unsymmetrical thiosulfonates as potential Alzheimer's disease therapeutics: In vitro and in silico study.Bioorganic & medicinal chemistry, , 06-15, Volume: 40, 2021
Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HTEuropean journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease.Bioorganic & medicinal chemistry, , 11-15, Volume: 28, Issue:22, 2020
Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , May-15, Volume: 194, 2020
Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Indazolylketones as new multitarget cannabinoid drugs.European journal of medicinal chemistry, , Mar-15, Volume: 166, 2019
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Design and development of molecular hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles as potential multifunctional agents to treat Alzheimer's disease.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Highly Selective Butyrylcholinesterase Inhibitors with Tunable Duration of Action by Chemical Modification of Transferable Carbamate Units Exhibit Pronounced Neuroprotective Effect in an Alzheimer's Disease Mouse Model.Journal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
[no title available]European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Discovery and Structure-Activity Relationships of a Highly Selective Butyrylcholinesterase Inhibitor by Structure-Based Virtual Screening.Journal of medicinal chemistry, , 08-25, Volume: 59, Issue:16, 2016
Design, synthesis and pharmacological evaluation of chalcone derivatives as acetylcholinesterase inhibitors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.Bioorganic & medicinal chemistry, , Jan-01, Volume: 21, Issue:1, 2013
The First Dual ChE/FAAH Inhibitors: New Perspectives for Alzheimer's Disease?ACS medicinal chemistry letters, , Mar-08, Volume: 3, Issue:3, 2012
(+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.European journal of medicinal chemistry, , Volume: 46, Issue:11, 2011
Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Benzofuran-based hybrid compounds for the inhibition of cholinesterase activity, beta amyloid aggregation, and abeta neurotoxicity.Journal of medicinal chemistry, , May-22, Volume: 51, Issue:10, 2008
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.Journal of medicinal chemistry, , Sep-10, Volume: 52, Issue:17, 2009
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.Journal of medicinal chemistry, , Oct-04, Volume: 50, Issue:20, 2007
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 43, 2021
Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.Journal of medicinal chemistry, , Aug-28, Volume: 57, Issue:16, 2014
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Bis-cycloSal-d4T-monophosphates: drugs that deliver two molecules of bioactive nucleotides.Journal of medicinal chemistry, , Mar-22, Volume: 50, Issue:6, 2007
Interaction of cycloSal-pronucleotides with cholinesterases from different origins. A structure-activity relationship.Journal of medicinal chemistry, , May-20, Volume: 47, Issue:11, 2004
Synthesis, crystal structure and biological evaluation of some novel 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines.European journal of medicinal chemistry, , May-06, Volume: 78, 2014
Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 72, 2022
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.Journal of natural products, , 02-22, Volume: 82, Issue:2, 2019
2,4-Disubstituted quinazolines as amyloid-β aggregation inhibitors with dual cholinesterase inhibition and antioxidant properties: Development and structure-activity relationship (SAR) studies.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Synthesis, in vitro pharmacology, and molecular modeling of syn-huprines as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Dec-20, Volume: 44, Issue:26, 2001
Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 27, Issue:22, 2017
Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.Journal of medicinal chemistry, , 01-11, Volume: 61, Issue:1, 2018
Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Homodimeric tacrine congeners as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
A review on coumarins as acetylcholinesterase inhibitors for Alzheimer's disease.Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl]phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Quinones bearing non-steroidal anti-inflammatory fragments as multitarget ligands for Alzheimer's disease.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
Synthesis of monomeric derivatives to probe memoquin's bivalent interactions.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.European journal of medicinal chemistry, , Volume: 46, Issue:11, 2011
Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Advancement of multi-target drug discoveries and promising applications in the field of Alzheimer's disease.European journal of medicinal chemistry, , May-01, Volume: 169, 2019
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Jan-04, Volume: 44, Issue:1, 2001
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
[no title available]Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease.Journal of medicinal chemistry, , 03-24, Volume: 65, Issue:6, 2022
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 43, 2021
Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6.Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.Journal of medicinal chemistry, , Sep-10, Volume: 52, Issue:17, 2009
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones.Bioorganic & medicinal chemistry, , Jan-01, Volume: 15, Issue:1, 2007
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.European journal of medicinal chemistry, , Volume: 46, Issue:11, 2011
Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Rational approach to discover multipotent anti-Alzheimer drugs.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 30, Issue:3, 2020
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).Bioorganic & medicinal chemistry, , 03-15, Volume: 27, Issue:6, 2019
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.Journal of medicinal chemistry, , Dec-26, Volume: 57, Issue:24, 2014
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's diJournal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Preparation, in vitro screening and molecular modelling of symmetrical 4-tert-butylpyridinium cholinesterase inhibitors--analogues of SAD-128.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Enables
This protein enables 9 target(s):
| Target | Category | Definition |
|---|
| amyloid-beta binding | molecular function | Binding to an amyloid-beta peptide/protein. [GOC:hjd] |
| catalytic activity | molecular function | Catalysis of a biochemical reaction at physiological temperatures. In biologically catalyzed reactions, the reactants are known as substrates, and the catalysts are naturally occurring macromolecular substances known as enzymes. Enzymes possess specific binding sites for substrates, and are usually composed wholly or largely of protein, but RNA that has catalytic activity (ribozyme) is often also regarded as enzymatic. [GOC:vw, ISBN:0198506732] |
| acetylcholinesterase activity | molecular function | Catalysis of the reaction: acetylcholine + H2O = choline + acetate. [EC:3.1.1.7] |
| cholinesterase activity | molecular function | Catalysis of the reaction: an acylcholine + H2O = choline + a carboxylic acid anion. [EC:3.1.1.8] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| hydrolase activity, acting on ester bonds | molecular function | Catalysis of the hydrolysis of any ester bond. [GOC:jl] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| choline binding | molecular function | Binding to choline, the amine 2-hydroxy-N,N,N-trimethylethanaminium. [GOC:mlg] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| nuclear envelope lumen | cellular component | The region between the two lipid bilayers of the nuclear envelope; 20-40 nm wide. [GOC:ai] |
| endoplasmic reticulum lumen | cellular component | The volume enclosed by the membranes of the endoplasmic reticulum. [ISBN:0198547684] |
| blood microparticle | cellular component | A phospholipid microvesicle that is derived from any of several cell types, such as platelets, blood cells, endothelial cells, or others, and contains membrane receptors as well as other proteins characteristic of the parental cell. Microparticles are heterogeneous in size, and are characterized as microvesicles free of nucleic acids. [GOC:BHF, GOC:mah, PMID:16373184] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
Involved In
This protein is involved in 12 target(s):
| Target | Category | Definition |
|---|
| xenobiotic metabolic process | biological process | The chemical reactions and pathways involving a xenobiotic compound, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:cab2, GOC:krc] |
| learning | biological process | Any process in an organism in which a relatively long-lasting adaptive behavioral change occurs as the result of experience. [ISBN:0582227089, ISBN:0721662544] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| neuroblast differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a neuroblast. There are at least four stages through which the pluripotent cells of epiblast or blastula become neuroblasts. [GOC:ef, ISBN:0878932585] |
| peptide hormone processing | biological process | The generation of a mature peptide hormone by posttranslational processing of a prohormone. [GOC:mah] |
| response to alkaloid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an alkaloid stimulus. Alkaloids are a large group of nitrogenous substances found in naturally in plants, many of which have extracts that are pharmacologically active. [GOC:jl] |
| cocaine metabolic process | biological process | The chemical reactions and pathways involving cocaine, an alkaloid obtained from the dried leaves of the shrub Erythroxylon coca. It is a cerebral stimulant and narcotic. [ISBN:0198506732] |
| negative regulation of synaptic transmission | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of synaptic transmission, the process of communication from a neuron to a target (neuron, muscle, or secretory cell) across a synapse. [GOC:ai] |
| response to glucocorticoid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a glucocorticoid stimulus. Glucocorticoids are hormonal C21 corticosteroids synthesized from cholesterol with the ability to bind with the cortisol receptor and trigger similar effects. Glucocorticoids act primarily on carbohydrate and protein metabolism, and have anti-inflammatory effects. [GOC:ai, PMID:9884123] |
| response to folic acid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a folic acid stimulus. [GOC:ai] |
| choline metabolic process | biological process | The chemical reactions and pathways involving choline (2-hydroxyethyltrimethylammonium), an amino alcohol that occurs widely in living organisms as a constituent of certain types of phospholipids and in the neurotransmitter acetylcholine. [GOC:jl, ISBN:0192801023] |
| acetylcholine catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of acetylcholine, the acetic acid ester of the organic base choline. [GOC:jl, ISBN:0192800752] |