Donepezil is a cholinesterase inhibitor used to treat mild to moderate Alzheimer’s disease. It works by increasing levels of acetylcholine, a neurotransmitter that plays a role in memory and learning. Donepezil is synthesized through a multi-step process involving a series of chemical reactions. It is a highly selective inhibitor of acetylcholinesterase, an enzyme that breaks down acetylcholine in the brain. This selective inhibition leads to an increase in acetylcholine levels, potentially improving cognitive function in Alzheimer's patients. Donepezil has been shown to improve cognitive function in patients with mild to moderate Alzheimer's disease, including memory, attention, and language skills. Its effectiveness in improving cognitive function and slowing disease progression has made it a widely prescribed medication for Alzheimer's disease. Researchers continue to study donepezil to investigate its potential benefits in other neurodegenerative disorders and to optimize its efficacy and safety. '
Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 3152 |
| CHEMBL ID | 502 |
| CHEBI ID | 145499 |
| CHEBI ID | 53289 |
| SCHEMBL ID | 2149 |
| SCHEMBL ID | 8265876 |
| MeSH ID | M0206795 |
| Synonym |
|---|
| AC-6969 |
| AB00640013-08 |
| AB00640013-07 |
| SPECTRUM5_001662 |
| aricept |
| donepezil [inn:ban] |
| 1h-inden-1-one, 2,3-dihydro-5,6-dimethoxy-2-((1-(phenylmethyl)-4-piperidinyl)methyl)- |
| SPECTRUM_001664 |
| OPREA1_188452 |
| e2020 |
| donepezil |
| 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1h-inden-1-one |
| domepezil |
| chembl502 , |
| bdbm8960 |
| (+/-)-2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-indan-1-one |
| DB00843 |
| KBIOSS_002144 |
| KBIO2_002144 |
| KBIO2_004712 |
| KBIO2_007280 |
| NCGC00167537-01 |
| AKOS000277311 |
| donaz |
| d-797 |
| donepezil (inn) |
| donaz (tn) |
| D07869 |
| 120014-06-4 |
| 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one |
| CHEBI:145499 |
| 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one |
| donepezilo |
| donepezilum |
| chebi:53289 , |
| STK003905 |
| 2-[(1-benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one |
| 8ssc91326p , |
| unii-8ssc91326p |
| hsdb 7743 |
| BCP9000622 |
| 142057-79-2 |
| 2-((1-benzylpiperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydro-1h-inden-1-one |
| BCPP000253 |
| nsc 737535 |
| nsc 758882 |
| FT-0601545 |
| S5073 |
| 5,6-dimethoxy-2-[[1-(phenylmethyl)piperidin-4-yl]methyl]-2,3-dihydroinden-1-one |
| gtpl6599 |
| 5,6-dimethoxy-2-((1-(phenylmethyl)-4-piperidinyl)methyl)-2,3-dihydro-1h-inden-1-one |
| donepezil [jan] |
| donepezil [mi] |
| d797 |
| donepezil [vandf] |
| donepezil [hsdb] |
| 2,3-dihydro-5,6-dimethoxy-2-((1-(phenylmethyl)-4-piperidinyl)methyl)-1h-inden-1-one |
| donepezil [who-dd] |
| (+/-)-2-((1-benzyl-4-piperidyl)methyl)-5,6-dimethoxy-1-indanone |
| donepezil [inn] |
| HY-14566 |
| 2,3-dihydro-5,6-dimethoxy-2 [[1-(phenyl methyl)-4-piperidinyl]methyl]-1h-inden-1-one |
| 2,3-dihydro-5,6-dimethoxy-2[[1-(phenyl methyl)-4-piperidinyl]methyl]-1h-inden-1-one |
| SCHEMBL2149 |
| DTXSID8048317 , |
| SCHEMBL8265876 |
| Q-100098 |
| 2-[(1-benzyl-4-piperidyl)methyl]- 5,6-dimethoxy-2,3-dihydroinden-1-one |
| AB00640013_09 |
| AB00640013_10 |
| mfcd00912833 |
| Z1741977105 |
| donepezil; 2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1h-inden-1-one; 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine; (+/-)-e 2020 |
| 2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1h-inden-1-one |
| SBI-0206789.P001 |
| MRF-0000323 |
| BCP07590 |
| Q415081 |
| 2-((1-benzyl-4-piperidyl)methyl)-5,6-dimethoxy-2,3-dihydroinden-1-one |
| BRD-A49160188-003-04-4 |
| 1h-inden-1-one, 2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]- |
| HMS3886M11 |
| AMY8939 |
| CCG-268401 |
| AKOS016842349 |
| (rs)-2-[(1-benzyl-4-piperidyl)methyl]-5,6-dimethoxyindan-1-one |
| EN300-267872 |
| 1h-inden-1-one,2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-,(2s)- |
| donepezil hydrochlorid |
| dtxcid0028292 |
| n06da02 |
Donepezil (DPZ) is a well-known drug for Alzheimer's disease that inhibits acetylcholinesterase activity (AChE) Donepezil is currently used in patients with mild to moderate AD, and has recently been shown to improve cognitive performance.
Donepezil has a neuroprotective effect against oxygen-glucose deprivation injury and glutamate toxicity in cultured cortical neurons. It has a significant effect in improving the ability of auditory comprehension, naming, repetition and oral expression.
Donepezil (DNPZ) has shown neuroprotective effect in many disorders. Donepezil has been approved, and higher dosages are recommended for the treatment of Alzheimer disease (AD)
Donepezil does not cause liver toxicity or significant drug interactions and is relatively well-tolerated. Donepezil can increase the amount of time that children with an ASD spend in the REM sleep state. It can activate AMPK and exerts neuroprotective effects.
Donepezil-treated MI rats were randomly assigned to the following four groups: peripheral infusion of saline (SPDT) or an α7-nAChR antagonist methyllycaconitine (α7PDT) or brain infusion of. saline (SBDT) Donepezil treatment protected rats from renal dysfunction in a dose-dependent manner.
Donepezil is an effective and safe drug for the long-term symptomatic treatment of mild to moderately severe AD for up to 144 weeks (2.5 years) Adverse events were more common with donepezil but mostly mild/moderate in severity. Across trials, the incidence of adverse events was generally lowest for dopezil and highest for rivastigmine.
The pharmacokinetic disposition of donepezil was observed to be both linear and dose proportional following single-dose administration. Data from 19 subjects who completed the study indicated no significant pharmacokinetics interactions between a single dose of memantine and multiple doses ofdonepezil. The assay method also shows good specificity to didpezil enantiomers.
Gunao-Yizhi decoction combined with donepezil has a significant prevalence in the treatment of vascular dementia, with no increase in adverse events. The treatment of the intervention group includes acupuncture combined with trad.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Therefore, its combination with acetylcholinesterase inhibitors (AChEIs) is anticipated." | ( Tolerability of memantine in combination with cholinesterase inhibitors in dementia therapy. Hartmann, S; Möbius, HJ, 2003) | 0.32 |
| " These results demonstrate that the PET imaging technique with specific labeled compounds in combination with microdialysis and a behavioral cognition task could be a useful method to clarify the mechanism of drugs in the living brains of experimental animals." | ( Effects of acute acetylcholinesterase inhibition on the cerebral cholinergic neuronal system and cognitive function: Functional imaging of the conscious monkey brain using animal PET in combination with microdialysis. Fukumoto, D; Kakiuchi, T; Nishiyama, S; Ohba, H; Sato, K; Tsukada, H, 2004) | 0.32 |
| "Reality orientation therapy combined with cholinesterase inhibitors has not been evaluated in patients with Alzheimer's disease." | ( Reality orientation therapy combined with cholinesterase inhibitors in Alzheimer's disease: randomised controlled trial. Bartorelli, L; Bernabei, R; Carbone, G; Frisoni, GB; Giacobini, E; Lambertucci, P; Onder, G; Silveri, MC; Zanetti, O, 2005) | 0.33 |
| "To study the efficacy and safety of Reinhartdt and sea cucumber capsule (RSC) combined with donepezil in treating Alzheimer's disease (AD), and its effect on thyroid function axis." | ( [Clinical study of Reinhartdt and sea cucumber capsule combined with donepezil in treating Alzheimer's disease]. Liang, LZ; Yan, YX; Zhou, ZL, 2007) | 0.79 |
| "Sixty-eight patients were randomly assigned to the RSC group, the Donepezil group and the combined treatment group, who were treated for 3 and 6 months with RSC, Donepezil and RSC combined with Donepezil, respectively." | ( [Clinical study of Reinhartdt and sea cucumber capsule combined with donepezil in treating Alzheimer's disease]. Liang, LZ; Yan, YX; Zhou, ZL, 2007) | 0.81 |
| "RSC combined with Donepezil in treating AD is effective and safe with no evident adverse reaction, better than single drug treatment, which may be through influencing the metabolism of thyroid hormones to improve the cognition function of AD patients." | ( [Clinical study of Reinhartdt and sea cucumber capsule combined with donepezil in treating Alzheimer's disease]. Liang, LZ; Yan, YX; Zhou, ZL, 2007) | 0.91 |
| "Cholinesterase inhibitors (ChEIs) could be involved in several drug-drug interactions (DDIs) because of their complex pharmacodynamic and/or pharmacokinetic properties." | ( Drug interactions with cholinesterase inhibitors: an analysis of the French pharmacovigilance database and a comparison of two national drug formularies (Vidal, British National Formulary). Bagheri, H; Lapeyre-Mestre, M; Montrastruc, JL; Sommet, A; Tavassoli, N, 2007) | 0.34 |
| "To observe clinical therapeutic effect of acupuncture combined with Yizhi Jiannao Granules for treatment of Alzheimer's disease and its effects on intelligence, daily life and social activity ability." | ( [Clinical observation on acupuncture combined with Yizhi Jiannao granules for treatment of Alzheimer's disease]. Dong, KL; Peng, XW, 2009) | 0.35 |
| "Acupuncture combined with Yizhi Jiannao Granules has a significant therapeutic effect on Alzheimer's disease, which is better than that of Yizhi Jiannao Granules or Aricept." | ( [Clinical observation on acupuncture combined with Yizhi Jiannao granules for treatment of Alzheimer's disease]. Dong, KL; Peng, XW, 2009) | 0.35 |
| "Compared with the donepezil treatment in the patients with mild-to-moderate AD, our results suggest that donepezil combined with natural hirudin may improve the treatment effects in the ADL, BPSD and cognition of the patients." | ( Donepezil combined with natural hirudin improves the clinical symptoms of patients with mild-to-moderate Alzheimer's disease: a 20-week open-label pilot study. Li, DQ; Yang, H; Zhou, YP, 2012) | 2.16 |
| "To evaluate the cost effectiveness of genetic screening for the apolipoprotein (APOE) ε4 allele in combination with preventive donepezil treatment in comparison with the standard of care for amnestic mild cognitive impairment (AMCI) patients in Canada." | ( Genetic testing in combination with preventive donepezil treatment for patients with amnestic mild cognitive impairment: an exploratory economic evaluation of personalized medicine. Beca, J; Black, S; Djalalov, S; Hoch, JS; Moretti, M; Musa, Z; Saposnik, G; Siminovitch, K; Yong, J, 2012) | 0.84 |
| "Using presently available clinical evidence, this exploratory study illustrates that genetic testing combined with preventive donepezil treatment for AMCI patients may be economically attractive." | ( Genetic testing in combination with preventive donepezil treatment for patients with amnestic mild cognitive impairment: an exploratory economic evaluation of personalized medicine. Beca, J; Black, S; Djalalov, S; Hoch, JS; Moretti, M; Musa, Z; Saposnik, G; Siminovitch, K; Yong, J, 2012) | 0.84 |
| " In other words, the tissue distribution of drugs can be influenced by drug-drug interaction (DDI) at efflux transporters in certain tissues (local DDI) without any apparent change in plasma concentration (systemic DDI)." | ( Local Drug-Drug Interaction of Donepezil with Cilostazol at Breast Cancer Resistance Protein (ABCG2) Increases Drug Accumulation in Heart. Nakanishi, T; Shinozaki, K; Takeuchi, R; Tamai, I, 2016) | 0.72 |
| " To alleviate the pill burden and swallowing difficulties associated with the condition, a fixed drug combination of extended-release memantine and donepezil was developed." | ( Memantine and donepezil: a fixed drug combination for the treatment of moderate to severe Alzheimer's dementia. Owen, RT, 2016) | 0.99 |
| "A total of 334 participants with Alzheimer's disease will be randomly assigned to either an electroacupuncture combined with donepezil group or a donepezil group with a ratio of 1:1." | ( The effect of electroacupuncture combined with donepezil on cognitive function in Alzheimer's disease patients: study protocol for a randomized controlled trial. Bin, L; Feng, Q; Liu, Z; Peng, W; Xu, M; Zhou, J, 2017) | 0.92 |
| " After the 15-day treatment, the Morris water maze test, micro-PET(positron-emission tomography), H&E (haematoxylin and eosin) staining, and immunohistochemistry were used to study the differences between donepezil (SAMP8+D), acupuncture (SAMP8+MA), and donepezil combined with acupuncture (SAMP8+D+MA) therapy for the treatment of Alzheimer's disease." | ( Effects of manual acupuncture combined with donepezil in a mouse model of Alzheimer's disease. Jiang, J; Li, Y; Li, Z; Liu, G; Shi, S, 2019) | 0.96 |
| "To investigate the effect of electroacupuncture (EA) combined with Donepezil on learning-memory ability and gene expression of β-amyloid (Aβ) clearance-related factors in the hippocampus in senescence-accelerated mouse prone 8 (SAMP8) mice, so as to explore their synthetic effect in improving dementia of Alzheimer's disease (AD)．." | ( [Effect of electroacupuncture combined with Donepezil on learning-memory ability and expression of hippocampal β-amyloid clearance-related genes in SAMP8 mice]. An, HY; Li, XH; Qiu, L; Tang, CL; Wu, MJ; Yang, YH; Yang, ZX; Zhu, ZW, 2020) | 1.06 |
| " Additionally, Alzheimer's type dementia drugs are often given in combination with antiplatelet drugs such as cilostazol." | ( [Pharmacokinetics/Pharmacodynamic Analysis to Link Pharmacokinetics to Efficacy and Drug Interaction of Alzheimer's Disease Drugs]. Kiriyama, A, 2021) | 0.62 |
| "To observe the effects of Dengzhan Shengmai capsule combined with donepezil hydrochloride on cognitive function, daily living ability, and safety in patients with Alzheimer's disease." | ( Dengzhan shengmai capsule combined with donepezil hydrochloride in the treatment of Alzheimer's disease: preliminary findings, randomized and controlled clinical trial. He, XY; Huang, P; Xu, M, 2021) | 1.13 |
| "Dengzhan Shengmai capsule combined with donepezil hydrochloride can improve cognitive function and the living capacity of patients with Alzheimer's disease, reduce the production of neurotoxic substances NO and ET, and provide higher safety." | ( Dengzhan shengmai capsule combined with donepezil hydrochloride in the treatment of Alzheimer's disease: preliminary findings, randomized and controlled clinical trial. He, XY; Huang, P; Xu, M, 2021) | 1.16 |
| " Thus, we studied the efficacy of prophylactic use of memantine alone or in combination with clinically used reversible acetylcholinesterase inhibitors (pyridostigmine, donepezil, rivastigmine) against soman." | ( Memantine and Its Combination with Acetylcholinesterase Inhibitors in Pharmacological Pretreatment of Soman Poisoning in Mice. Karasova, JZ; Kassa, J, 2021) | 0.82 |
| "To explore the effect of resveratrol (RES) combined with donepezil hydrochloride on inflammatory factor level and cognitive function level of patients with Alzheimer's disease (AD)." | ( Effect of Resveratrol Combined with Donepezil Hydrochloride on Inflammatory Factor Level and Cognitive Function Level of Patients with Alzheimer's Disease. Fang, X; Wang, L; Zhang, J; Zhao, J, 2022) | 1.24 |
| " Therefore, meta-analysis is employed in this study to evaluate the efficacy and safety of using donepezil hydrochloride combined with nimodipine in treating VaD to provide references for clinical treatments." | ( A systematic review of the efficacy of donepezil hydrochloride combined with nimodipine on treating vascular dementia. Huang, KL; Liu, J; Ran, SM; Tan, AH; Wang, GY; Wang, MY; Yang, Q, 2022) | 1.21 |
| "Donepezil hydrochloride combined with nimodipine had demonstrated satisfactory efficacy on the treatment of vascular dementia." | ( A systematic review of the efficacy of donepezil hydrochloride combined with nimodipine on treating vascular dementia. Huang, KL; Liu, J; Ran, SM; Tan, AH; Wang, GY; Wang, MY; Yang, Q, 2022) | 2.43 |
| "Donepezil hydrochloride combined with nimodipine had good efficacy in the treatment of patients with vascular dementia, mainly in terms of improving the Simple MMSE scores, the ability to use daily living scale (ADL) scores and the CDR, and the best results were obtained after 12 weeks of intervention." | ( A systematic review of the efficacy of donepezil hydrochloride combined with nimodipine on treating vascular dementia. Huang, KL; Liu, J; Ran, SM; Tan, AH; Wang, GY; Wang, MY; Yang, Q, 2022) | 2.43 |
| " Existing evidence shows that acupuncture has advantages in the treatment of AD, but whether the efficacy of acupuncture belongs to the placebo effect remains controversial, and there is no strict placebo-controlled clinical study to evaluate the efficacy and safety of acupuncture combined with Western medicine in the treatment of AD." | ( Clinical efficacy of acupuncture combined with Western medicine in the treatment of mild to moderate Alzheimer disease: A protocol of a randomized controlled trial. Guo, R; He, J; Quan, L; Zhou, K, 2022) | 0.72 |
| "This is a prospective randomized, a single-blind, sham-acupuncture controlled trial to study the clinical efficacy of acupuncture combined with Western medicine in the treatment of mild to moderate AD." | ( Clinical efficacy of acupuncture combined with Western medicine in the treatment of mild to moderate Alzheimer disease: A protocol of a randomized controlled trial. Guo, R; He, J; Quan, L; Zhou, K, 2022) | 0.72 |
| "This study will evaluate the efficacy of acupuncture combined with Western medicine in improving cognitive function and activities of daily living in AD patients." | ( Clinical efficacy of acupuncture combined with Western medicine in the treatment of mild to moderate Alzheimer disease: A protocol of a randomized controlled trial. Guo, R; He, J; Quan, L; Zhou, K, 2022) | 0.72 |
| " This review conducted a systematic review of the current evidence on the efficacy and safety of Gunao-Yizhi decoction combined with donepezil for VaD." | ( Gunao-Yizhi decoction combined with donepezil for vascular dementia: A systematic review and meta-analysis. Bi, S; Guan, X; Hou, H; Hu, Y; Li, M; Liu, C; Wang, K; Zhang, L, 2022) | 1.2 |
| "China National Knowledge Infrastructure (CNKI), Wanfang database (Wanfang), Chinese Science and Technology Periodical Database (VIP), China Biology Medicine disc (CBM), MEDLINE, EMBASE, and Cochrane Library were searched for randomized controlled trials on Gunao-Yizhi decoction combined with donepezil for VaD." | ( Gunao-Yizhi decoction combined with donepezil for vascular dementia: A systematic review and meta-analysis. Bi, S; Guan, X; Hou, H; Hu, Y; Li, M; Liu, C; Wang, K; Zhang, L, 2022) | 1.17 |
| " Compared with donepezil alone, meta-analysis showed that Gunao-Yizhi decoction combined with donepezil could improve clinical efficacy, mini-mental state examination (MMSE) score, Hasegawa dementia scale (HDS), increase the level of superoxide dismutase (SOD) in serum, and reduce the level of malonaldehyde dismutas (MDA) in serum." | ( Gunao-Yizhi decoction combined with donepezil for vascular dementia: A systematic review and meta-analysis. Bi, S; Guan, X; Hou, H; Hu, Y; Li, M; Liu, C; Wang, K; Zhang, L, 2022) | 1.35 |
| "Gunao-Yizhi decoction combined with donepezil has a significant prevalence in the treatment of vascular dementia, with no increase in adverse events." | ( Gunao-Yizhi decoction combined with donepezil for vascular dementia: A systematic review and meta-analysis. Bi, S; Guan, X; Hou, H; Hu, Y; Li, M; Liu, C; Wang, K; Zhang, L, 2022) | 1.27 |
| "This study explored the feasibility and effectiveness of a short-term (10-week) intervention trial using Donepezil administered alone and combined with intensive language action therapy (ILAT) for the treatment of apathy and depression in ten people with chronic post-stroke aphasia." | ( Donepezil alone and combined with intensive language-action therapy on depression and apathy in chronic post-stroke aphasia: A feasibility study. Berthier, ML; Dávila, G; Edelkraut, L; Jorge, RE; López-Barroso, D; López-González, FJ; Mohr, B; Pulvermüller, F; Starkstein, SE; Torres-Prioris, MJ, 2023) | 2.57 |
| "The network meta-analysis was used to evaluate the efficacy of acupuncture combined with other therapies in the treatment of post stroke cognitive impairment (PSCI)." | ( The efficacy of acupuncture combined with other therapies in post stroke cognitive impairment: A network meta-analysis. Dong, X; Huo, H; Li, S; Liu, Y; Wang, D; Wang, Y; Zhang, H; Zhang, Y; Zhao, D, 2023) | 0.91 |
| " The treatment of the intervention group includes acupuncture combined with traditional Chinese medicine prescriptions (TCMP), acupuncture combined with hyperbaric oxygen (HBO), acupuncture combined with repetitive transcranial magnetic stimulation (rTMS), acupuncture combined with cognitive rehabilitation (CR), acupuncture combined with donepezil." | ( The efficacy of acupuncture combined with other therapies in post stroke cognitive impairment: A network meta-analysis. Dong, X; Huo, H; Li, S; Liu, Y; Wang, D; Wang, Y; Zhang, H; Zhang, Y; Zhao, D, 2023) | 1.08 |
| "Acupuncture combined with TCMP may be the best treatment method among all of the above treatments for PSCI." | ( The efficacy of acupuncture combined with other therapies in post stroke cognitive impairment: A network meta-analysis. Dong, X; Huo, H; Li, S; Liu, Y; Wang, D; Wang, Y; Zhang, H; Zhang, Y; Zhao, D, 2023) | 0.91 |
| " After drug treatment, the results showed that AD patients with HLJD combined with DON treatment didn't increase the adverse effects and had good compliance." | ( Efficacy evaluation and metabolomics analysis of Huanglian Jiedu decoction in combination with donepezil for Alzheimer's disease treatment. Huang, J; Xu, M; Yue, Y, 2023) | 1.13 |
No studies have reported cocaine bioavailability in human subjects receiving donepezil. The modulation of donepezill release from MIPs-based formulations using oil vehicles may contribute to decrease its side effects.
The current work is focused on developing mannose-coated PLGA nanoparticles for delivering Donepezil and Memantine in one dosage form. The variability associated with the dose-response analysis was attributable primarily to subject age, such that older monkeys required higher doses of donepezil.
| Excerpt | Relevance | Reference |
|---|---|---|
| " The reversal of scopolamine-induced impairment was characterized by the presence of an inverted U-shaped dose-response curve." | ( An inverted U-shaped curve for heptylphysostigmine on radial maze performance in rats: comparison with other cholinesterase inhibitors. Braida, D; Griffini, P; Lamperti, M; Maggi, A; Paladini, E; Sala, M, 1996) | 0.29 |
| "The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, and dosage and administration of donepezil are reviewed." | ( Donepezil: an anticholinesterase inhibitor for Alzheimer's disease. Shintani, EY; Uchida, KM, 1997) | 1.95 |
| " The reversal of scopolamine-induced impairment was characterized by an inverted U-shaped dose-response curve." | ( Long-lasting antiamnesic effect of a novel anticholinesterase inhibitor (MF268). Braida, D; Colibretti, L; Griffini, P; Lamperti, M; Paladini, E; Sala, M, 1998) | 0.3 |
| " Both dosage regimens were well tolerated; no clinically significant changes in laboratory or vital sign parameters were observed in any subject." | ( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following evening administration. Friedhoff, LT; Rogers, SL; Tiseo, PJ, 1998) | 0.56 |
| "The measured pharmacokinetic and pharmacodynamic parameters for both 5 and 10 mg day(-1) donepezil administered in the evening are in good agreement with previous results obtained with morning administration, indicating no time of dosing effect." | ( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following evening administration. Friedhoff, LT; Rogers, SL; Tiseo, PJ, 1998) | 0.78 |
| " These results suggest that the administration of donepezil to patients with hepatic disease in clinical practice should not require any dosing modifications." | ( An evaluation of the pharmacokinetics of donepezil HCl in patients with impaired hepatic function. Friedhoff, LT; Perdomo, CA; Tiseo, PJ; Vargas, R, 1998) | 0.82 |
| " Furthermore, its long half-life supports a simple and convenient once-daily dosing regimen." | ( Clinical profile of donepezil in the treatment of Alzheimer's disease. Doody, RS, 1999) | 0.63 |
| " A dose-response effect was evident, with the 10 mg/day donepezil group demonstrating greater benefits in all outcome measures than the 5 mg/day group." | ( The effects of donepezil in Alzheimer's disease - results from a multinational trial. Burns, A; Friedhoff, LT; Gauthier, S; Hecker, J; Möller, HJ; Petit, H; Rogers, SL; Rossor, M, ) | 0.73 |
| " These benefits, as well as a simple, once-daily dosing regimen, make donepezil a viable therapeutic option for AD patients." | ( Clinical benefits of a new piperidine-class AChE inhibitor. Doody, RS, 1999) | 0.54 |
| "To report toxicity resulting from donepezil administration following a tenfold dosing error." | ( Donepezil overdose: a tenfold dosing error. Edwards, R; Klein-Schwartz, W; Shepherd, G, ) | 1.85 |
| "A tenfold dosing error caused donepezil toxicity." | ( Donepezil overdose: a tenfold dosing error. Edwards, R; Klein-Schwartz, W; Shepherd, G, ) | 1.86 |
| " The first large-scale study designed to evaluate the efficacy of Aricept administered at a daily dosage of 5 to 10 mg was conducted over 14 weeks." | ( [Cholinergic hypothesis and Alzheimer's disease: the place of donepezil (Aricept)]. Bertogliati, C; Gokalsing, E; Robert, PH, 1999) | 0.54 |
| " Donepezil (5 and 10 mg) is an agent with a simple once-daily dosage schedule which improves cognition and global clinical function in the short (up to 24 weeks) and long term (up to about 1 year) in patients with mild to moderate Alzheimer's disease." | ( Donepezil: a review of its use in Alzheimer's disease. Dooley, M; Lamb, HM, 2000) | 2.66 |
| " The present study investigated the dose-response characteristics of donepezil, tacrine, rivastigmine and metrifonate in inducing tremor, lacrimation, salivation and hypothermia and the duration of action of these compounds in Lister hooded rats." | ( Comparison of donepezil-, tacrine-, rivastigmine- and metrifonate-induced central and peripheral cholinergically mediated responses in the rat. Dronfield, S; Egan, K; Green, AR; Marsden, CA, 2000) | 0.9 |
| " In order to maximize and prolong positive drug effects, it is important to start early and adjust dosage during the treatment." | ( Cholinesterase inhibitors stabilize Alzheimer's disease. Giacobini, E, 2000) | 0.31 |
| "Cholinesterase inhibitors (ChEIs) are dosed in two phases for the treatment of dementia, an initial dose-escalation phase to achieve a therapeutic dose and a maintenance phase where the therapeutic dose is given for long-term therapy." | ( The tolerability and safety of cholinesterase inhibitors in the treatment of dementia. Inglis, F, 2002) | 0.31 |
| " Beneficial effects in other similar patients or at higher dosage cannot be excluded." | ( An N-of-1 randomized controlled trial ('N-of-1 trial') of donepezil in the treatment of non-progressive amnestic syndrome. Grimley Evans, J; Price, JD, 2002) | 0.56 |
| " Improvement in behavioural symptoms also occurs, but without a dose-response relationship." | ( Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors. Jann, MW; Shirley, KL; Small, GW, 2002) | 0.31 |
| " Both medications were administered open label according to recommended dosing regimens from the respective product labelling available during the conduct of the study." | ( A multinational, randomised, 12-week, comparative study of donepezil and rivastigmine in patients with mild to moderate Alzheimer's disease. Bahra, RS; Bullock, R; Engelbrecht, I; Hock, C; Hopker, SW; Ieni, JR; Maud, CM; Passmore, AP; Potocnik, FC; Smith, R; Wilkinson, DG, ) | 0.37 |
| " The results indicate that no clinically meaningful drug interactions occurred between risperidone 1 mg daily and donepezil 5 mg daily at steady state, and therefore no dosage adjustment is required when both drugs are combined with the dosage regimen studied." | ( Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil. Jia, X; Parier, JL; Pesco-Koplowitz, L; Xie, C; Zhao, Q, 2003) | 0.75 |
| "1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg." | ( Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors. Albuquerque, EX; Christner, C; Fehrenbacher, A; Höffle, A; Jostock, R; Lübbert, H; Ludwig, J; Maelicke, A; Pereira, EF; Radina, M; Samochocki, M; Ullmer, C; Zerlin, M, 2003) | 0.32 |
| " A cumulative dose-response relationship was observed between longer-term sustained donepezil use and delay of NHP." | ( Donepezil is associated with delayed nursing home placement in patients with Alzheimer's disease. Geldmacher, DS; Ieni, JR; Mastey, V; McRae, T; Provenzano, G, 2003) | 1.99 |
| " It is important to prevent dosing errors in cooperation with medical providers, patients and families." | ( [A case of acute cholinergic adverse effects induced by donepezil overdose: a follow-up of clinical course and plasma concentration of donepezil]. Fukuhara, Y; Kowa, H; Nakashima, K; Wada, K; Yano, H, 2003) | 0.57 |
| "In this 12-week, open-label, multicentre trial, patients with probable mild-to-moderate Alzheimer's disease received donepezil 5 mg/day for 28 days, after which the dosage was increased to 10 mg/day according to the investigating clinician's judgement." | ( Efficacy and safety of donepezil in patients with Alzheimer's disease: results of a global, multinational, clinical experience study. Bahra, R; Baloyannis, S; Boada-Rovira, M; Brodaty, H; Cras, P; Emre, M; Zhang, R, 2004) | 0.84 |
| " Side effects were associated with dosage increases." | ( Randomized placebo-controlled trial of donepezil in cognitive impairment in Parkinson's disease. Brandt, J; Grill, S; Leroi, I; Lyketsos, CG; Marsh, L; Reich, SG; Thompson, R, 2004) | 0.59 |
| " However, variable tolerability in our sample underscores the need for careful monitoring when prescribing donepezil to patients with PD, especially with dosage increases." | ( Randomized placebo-controlled trial of donepezil in cognitive impairment in Parkinson's disease. Brandt, J; Grill, S; Leroi, I; Lyketsos, CG; Marsh, L; Reich, SG; Thompson, R, 2004) | 0.81 |
| " Dose-response curves for tremor (central effect) and salivation (peripheral effect) showed that donepezil and icopezil possess a more favourable therapeutic index than the nonselective inhibitors, tacrine and heptylphysostigmine." | ( Pharmacology of selective acetylcholinesterase inhibitors: implications for use in Alzheimer's disease. Chapin, D; Hubbard, ST; Jones, SB; Liston, DR; Nason, D; Nielsen, JA; Ramirez, A; Shalaby, IA; Villalobos, A; White, WF, 2004) | 0.54 |
| " Activities of daily living and social behaviour: On the Instrumental Activity of Daily Living (IADL) scale, there was no statistically significant difference between the groups taking donepezil 5mg per day donepezil and placebo, but the group taking 10 mg of donepezil a day showed benefit compared with placebo There were statistically significant benefit for donepezil at either dosage compared with placebo on the Alzheimer's Disease Functional Assessment and Change Scale (ADFACS)." | ( Donepezil for vascular cognitive impairment. Birks, J; Malouf, R, 2004) | 1.96 |
| " A prospective, randomized, placebo-controlled clinical trial with standard timing, dosage and treatment duration is recommended to further evaluate treatment efficacy." | ( The effects of Donepezil on traumatic brain injury acute rehabilitation outcomes. Cornis-Pop, M; Gibellato, M; Jena, T; Lew, H; Seel, R; Silver, T; Walker, W, 2004) | 0.68 |
| "The authors estimated the effects of each of the three commonly used drugs for Alzheimer disease (donepezil, galantamine, and rivastigmine) in terms of predefined clinical outcomes and trial completion rates, by dosing level, and described differences among them." | ( Metaanalysis of randomized trials of the efficacy and safety of donepezil, galantamine, and rivastigmine for the treatment of Alzheimer disease. Ames, D; Clayton, T; Lai, R; Ritchie, CW, ) | 0.59 |
| " Beginning on day 22, the donepezil dosage was doubled for 22 days to the target dose of 10 mg once daily, with the last donepezil dose concomitantly administered with memantine 10 mg on day 43." | ( Lack of pharmacokinetic or pharmacodynamic interaction between memantine and donepezil. Abramowitz, WT; Periclou, AP; Rao, N; Sherman, T; Ventura, D, 2004) | 0.85 |
| " The variability associated with the dose-response analysis was attributable primarily to subject age, such that older monkeys required higher doses of donepezil." | ( Donepezil-induced improvement in delayed matching accuracy by young and old rhesus monkeys. Buccafusco, JJ; Terry, AV, 2004) | 1.96 |
| " At concentrations that include their prescribed dosage ranges, donepezil (1-1000 nM) and galantamine (50-1000 nM) increase action potential-dependent dopamine release." | ( Cholinergic drugs for Alzheimer's disease enhance in vitro dopamine release. Dani, JA; Zhang, L; Zhou, FM, 2004) | 0.56 |
| " Three head-to-head trials of ChEIs in the treatment of AD have been published to date, but are limited due to their open-label design, rates of titration, and the drug dosage levels utilised." | ( The benefits and risks associated with cholinesterase inhibitor therapy in Alzheimer's disease. Herrmann, N; Lanctôt, KL; Thompson, S, 2004) | 0.32 |
| " Although insomnia and other sleep disorders have been reported following administration of donepezil, lengthening the time period before increasing the dose of donepezil from 5 to 10 mg day(-1) or switching to morning dosing can reduce these events to the levels of placebo-treated patients." | ( The safety and tolerability of donepezil in patients with Alzheimer's disease. Ham, RJ; Jackson, S; Wilkinson, D, 2004) | 0.83 |
| "These results indicate that the pharmacokinetics of donepezil are not altered after dosing to steady state, and that donepezil can be administered safely to subjects with moderate renal impairment." | ( Steady-state pharmacokinetics and safety of donepezil HCl in subjects with moderately impaired renal function. Bolton, WK; Cullen, EI; Gutierrez, MJ; Hutman, HW; Kumar, D; Marbury, TC; Nagy, CF; Pratt, RD, 2004) | 0.84 |
| " In consecutive dosing periods separated by washout periods of > or = 3 weeks, healthy volunteers received either oral donepezil HCI 5 mg once daily for 15 days, oral sertraline HCl 50 mg once daily for 5 days followed by 10 days of once-daily sertraline HCl 100 mg, or the simultaneous administration of oral donepezil HCl and sertraline HCl." | ( Concurrent administration of donepezil HCl and sertraline HCl in healthy volunteers: assessment of pharmacokinetic changes and safety following single and multiple oral doses. Cullen, EI; Kumar, D; Nagy, CF; Perdomo, CA; Pratt, RD; Wason, S, 2004) | 0.82 |
| "Repeated dosing with donepezil, 5 mg daily for 2 weeks, had no significant effect on the safety, tolerability or pharmacokinetics of thioridazine." | ( Repeated dosing with donepezil does not affect the safety, tolerability or pharmacokinetics of single-dose thioridazine in young volunteers. Boyce, M; Dunn, K; Johnston, A; Ravic, M; Warrington, S, 2004) | 0.96 |
| "Twenty-five patients with PD who were taking physician-optimized doses of levodopa/carbidopa (with daytime dosing intervals of 4-8 h) were administered once-daily doses of either donepezil HCl (5 mg) or placebo for 15 days, in two treatment periods, separated by a washout of at least 2 weeks." | ( Concurrent administration of donepezil HCl and levodopa/carbidopa in patients with Parkinson's disease: assessment of pharmacokinetic changes and safety following multiple oral doses. Cullen, EI; Hahne, WA; Kirby, L; Kumar, D; Okereke, CS; Pratt, RD, 2004) | 0.81 |
| "These results suggest that once-daily dosing of 5 mg donepezil HCl does not alter the PK of risperidone in patients with schizophrenia." | ( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses. Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004) | 0.86 |
| " Nefiracetam has been shown to potentiate ACh currents in the alpha4beta2 receptor of rat cortical neurons with a bell-shaped dose-response relationship and the maximum effect at 1 nM." | ( Mechanisms of action of cognitive enhancers on neuroreceptors. Marszalec, W; Moriguchi, S; Narahashi, T; Yeh, JZ; Zhao, X, 2004) | 0.32 |
| " Higher dosages often did not exert beneficial effects in accordance with inverted U-shaped dose-response curves described for cholinomimetics." | ( Symptomatic effect of donepezil, rivastigmine, galantamine and memantine on cognitive deficits in the APP23 model. Abramowski, D; De Deyn, PP; Staufenbiel, M; Van Dam, D, 2005) | 0.64 |
| "54 mg kg-1 D-1 dosage as a positive control drug, DZXYS in 12." | ( [Protective effect of Danzhi-xiaoyao San on rat brain energy or material metabolism (correction of matebolism) dealt with D-galactose]. Cai, DY; Chen, JX; Huang, QF; Sun, LP; Wang, X; Zhang, JJ; Zhang, W, 2005) | 0.33 |
| " The author provides information on recommended dosing for all three medications, noting that cholinesterase inhibitors must be titrated carefully." | ( Cholinesterase inhibitors in the treatment of dementia. Ellis, JM, 2005) | 0.33 |
| " Initially, we established a dose-response relationship for the acute and chronic haloperidol and DOI-induced HTR." | ( Effects of donepezil, nicotine and haloperidol on the central serotonergic system in mice: implications for Tourette's syndrome. Hayslett, RL; Tizabi, Y, 2005) | 0.72 |
| " The drug was administered at a dosage of 5 mg/day for 1 month and 10 mg/day for the following 7 months, as tolerated." | ( Cardiovascular effects and risk of syncope related to donepezil in patients with Alzheimer's disease. Bordier, P; Garrigue, S; Gencel, L; Lafitte, A; Lanusse, S; Margaine, J; Robert, F, 2006) | 0.58 |
| "This study compared dosing and utilization patterns of the cholinesterase inhibitors (ChEIs) donepezil, rivastigmine, and galantamine in the nursing home setting." | ( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis. Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006) | 0.55 |
| " The mean daily dosage of donepezil was above the effective dose throughout the study period, whereas the mean daily dosage was below the effective dose for the first 3 months with rivastigmine and did not approach the effective dose for galantamine until month 12." | ( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis. Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006) | 0.63 |
| "The results of this study suggest that early effective dosing occurred more often with donepezil than with rivastigmine or galantamine in these nursing home residents." | ( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis. Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006) | 0.56 |
| "Patients enrolled in the present study had a 6-week single-blind placebo washout period followed by treatment with donepezil 5 mg/day for 6 weeks with an optional increase in dosage to 10 mg/day between weeks 6 and 32." | ( Efficacy and safety of donepezil over 3 years: an open-label, multicentre study in patients with Alzheimer's disease. Burns, A; Gauthier, S; Perdomo, C, 2007) | 0.86 |
| " Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process." | ( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A, ) | 0.13 |
| " An unexpectedly large placebo effect, inadequate dosage (mean 120 mg/day), and inadequate power may have contributed to lack of demonstrable benefit." | ( Quetiapine for agitation or psychosis in patients with dementia and parkinsonism. Cummings, J; Kurlan, R; Raman, R; Thal, L, 2007) | 0.34 |
| " Further investigation would be required to determine whether individual patients, or those with particular epilepsy syndromes, might benefit from donepezil or other acetylcholinesterase inhibitors, or if a higher dosage might be effective." | ( A randomized, double-blind, placebo-controlled trial of donepezil to improve memory in epilepsy. Choi, H; Hamberger, MJ; Hirsch, LJ; Palmese, CA; Scarmeas, N; Weintraub, D, 2007) | 0.79 |
| " Nevertheless, whereas in the case of donepezil there seems to be a positive relation between the maximum dosage and response, for galanthamine doses above 24 mg/day do not seem to offer any improvement." | ( [Galanthamine versus donepezil in the treatment of Alzheimer's disease]. Garre-Olmo, J; López-Pousa, S; Vilalta-Franch, J, ) | 0.72 |
| " Tolerability can be increased by use of flexible dosing and efficacy is likely to be enhanced by increasing the length of the trial from six to 12 months and by enriching the sample with subjects more likely to decline during the trial." | ( Key lessons learned from short-term treatment trials of cholinesterase inhibitors for amnestic MCI. Correia, S; Richardson, S; Salloway, S, 2008) | 0.35 |
| " When administered 20 min before acquisition, memantine elicited an inverted U-shape dose-response relationship, with low doses (0." | ( The uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist memantine prolongs spatial memory in a rat delayed radial-arm maze memory task. Lichtman, AH; Wise, LE, 2007) | 0.34 |
| " At week 6 of randomization, the dosage of donepezil was increased to 10 mg/d." | ( A double-blind, placebo-controlled trial of donepezil for the treatment of menopause-related cognitive loss. Devi, G; Khosrowshahi, L; Laakso, UK; Massimi, S; Schultz, S, 2007) | 0.86 |
| " A statistically significant dose-response relationship was demonstrated with the SIB and CIBIC-plus." | ( Donepezil treatment of patients with severe Alzheimer's disease in a Japanese population: results from a 24-week, double-blind, placebo-controlled, randomized trial. Arimoto, I; Asada, T; Homma, A; Imai, Y; Iwamoto, T; Koma, H; Ohbayashi, T; Shigeta, M; Tago, H; Takita, M, 2008) | 1.79 |
| "This study confirmed the effectiveness of donepezil 10 mg/day in patients with severe AD and demonstrated a significant dose-response relationship." | ( Donepezil treatment of patients with severe Alzheimer's disease in a Japanese population: results from a 24-week, double-blind, placebo-controlled, randomized trial. Arimoto, I; Asada, T; Homma, A; Imai, Y; Iwamoto, T; Koma, H; Ohbayashi, T; Shigeta, M; Tago, H; Takita, M, 2008) | 2.05 |
| " We determine the effects of sub-chronic dosing of ChEIs on alpha7 and non-alpha7 nAChRs and determine if differences can be observed between them." | ( Effects of cholinesterase inhibitors on rat nicotinic receptor levels in vivo and in vitro. Reid, RT; Sabbagh, MN, 2008) | 0.35 |
| " Dose-response curves of donepezil effect both on I (C) and I (K) were shifted right along horizontal axis when donepezil was applied in combination with TEA." | ( The binding of donepezil with external mouth of K+-channels of molluscan neurons. Bukanova, JV; Marchenko, EV; Rossokhin, AV; Skrebitsky, VG; Solntseva, EI, 2009) | 1.01 |
| " The dosage rose to 10 mg daily for another 6 weeks before a 2-week course of cognitive training and was maintained for the remainder of a year." | ( Acetylcholinesterase inhibitor in combination with cognitive training in older adults. Ashford, JW; Friedman, L; Hoblyn, J; Kraemer, HC; Mumenthaler, MS; Noda, A; Yesavage, JA, 2008) | 0.35 |
| " A dose-response effect was observed for donepezil, with the highest-dose group at greatest risk (HR=2." | ( Cholinesterase inhibitors and incidence of bradycardia in patients with dementia in the veterans affairs new England healthcare system. Cantor, MD; Farwell, W; Hernandez, RK; Lawler, EV, 2009) | 0.62 |
| "05) tests as compared to those dosed with the vehicle." | ( Metabolic profiling of rat brain and cognitive behavioral tasks: potential complementary strategies in preclinical cognition enhancement research. Atcha, Z; Aw, CC; Browne, ER; Chan, EC; Chen, WS; Goh, CW; Goh, DP; Neo, AH; New, LS, 2009) | 0.35 |
| " Donepezil was orally given at a dosage of 5 mgxkg(-1)xday(-1)." | ( Anti-Alzheimer's drug, donepezil, markedly improves long-term survival after chronic heart failure in mice. Ando, M; Arikawa, M; Handa, T; Kakinuma, Y; Katare, RG; Sasaguri, S; Sato, T; Yamasaki, F, 2009) | 1.57 |
| " The results showed that piperine at all dosage range used in this study significantly improved memory impairment and neurodegeneration in hippocampus." | ( Piperine, the main alkaloid of Thai black pepper, protects against neurodegeneration and cognitive impairment in animal model of cognitive deficit like condition of Alzheimer's disease. Chonpathompikunlert, P; Muchimapura, S; Wattanathorn, J, 2010) | 0.36 |
| " Repeated (3 days) daily dosing of ABT-107 increased extracellular cortical acetylcholine in rats, whereas acute administration increased cortical extracellular signal-regulated kinase and cAMP response element-binding protein phosphorylation in mice, neurochemical and biochemical events germane to cognitive function." | ( In vivo pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107: preclinical considerations in Alzheimer's disease. Anderson, DJ; Bitner, RS; Browman, K; Buccafusco, J; Bunnelle, WH; Decker, MW; Drescher, KU; Gopalakrishnan, M; Kohlhaas, KL; Markosyan, S; Marsh, KC; Nikkel, AL; Radek, R, 2010) | 0.36 |
| " The aim of this study was to assess an alternative oral dosing method that could reduce the distress and morbidity associated with standard gavage techniques." | ( Alternative method of oral dosing for rats. Atcha, Z; Aw, CC; Browne, ER; Goh, CW; Lim, JS; Neo, AH; Pemberton, DJ; Rourke, C, 2010) | 0.36 |
| " For 10 mg and 5 mg donepezil once-daily dosing, the estimated forgiveness of donepezil was 80% and 90% daily compliance or two and one dosage omissions at steady state, respectively." | ( Compliance assessment of ambulatory Alzheimer patients to aid therapeutic decisions by healthcare professionals. Freiberg, I; Kloft, C; Scheerans, C; Schmidt-Pokrzywniak, A; Schwalbe, O; Stang, A, 2010) | 0.68 |
| " The dosage of ChEI treatment could possibly lead to a different functional outcome." | ( Long-term outcome and prediction models of activities of daily living in Alzheimer disease with cholinesterase inhibitor treatment. Londos, E; Minthon, L; Wallin, ÅK; Wattmo, C, ) | 0.13 |
| " A higher oral dosage was suggested to have a better therapeutic response in reported results, but the plasma concentration of donepezil was not examined with respect to the therapeutic outcomes in those studies." | ( Plasma concentration of donepezil to the therapeutic response of Alzheimer's disease in Taiwanese. Chen, SH; Chou, MC; Lai, CL; Liu, CK; Wu, SL; Yang, YH, 2011) | 0.88 |
| " Experiment 1 tested the effects of 5 mg/per day dosage on cognitive and EEG markers at 6-hour, 2-week and 4-week follow-ups." | ( Donepezil impairs memory in healthy older subjects: behavioural, EEG and simultaneous EEG/fMRI biomarkers. Balsters, JH; Bokde, AL; Brennan, S; Cassidy, SM; Delmonte, S; Fagan, AJ; Galli, A; Kilcullen, SM; Lai, R; Laruelle, M; Lawlor, B; Martin, MP; Meaney, JF; O'Connell, RG; Robertson, IH; Upton, N, 2011) | 1.81 |
| " Change of LTP by donepezil treatment had a bell-shaped dose-response curve." | ( Donepezil in a narrow concentration range augments control and impaired by beta-amyloid peptide hippocampal LTP in NMDAR-independent manner. Bukanova, JV; Kapai, NA; Skrebitsky, VG; Solntseva, EI, 2012) | 2.16 |
| " The dosage was one tablet/day (5 mg) for the first two weeks and two tablets/day (10 mg) for the last two weeks." | ( Beneficial effect of donepezil on obstructive sleep apnea: a double-blind, placebo-controlled clinical trial. Guilleminault, C; Moraes, W; Poyares, D; Sukys-Claudino, L; Tufik, S, 2012) | 0.7 |
| "This sequence of dosage and symptoms suggests acetylcholinesterase inhibition was the trigger for release of these memories, which are otherwise mostly chronically repressed in this individual." | ( Case report: Post-traumatic memories triggered by donepezil in a dose-dependent pattern. Wolff, ML, 2012) | 0.63 |
| " CBF was measured by laser Doppler from rat cerebral cortex after 8 weeks of daily oral dosing of these drugs." | ( Bacopa monnieri increases cerebral blood flow in rat independent of blood pressure. Chootip, K; Ingkaninan, K; Kamkaew, N; Norman Scholfield, C; Taepavarapruk, N, 2013) | 0.39 |
| "0) on stable donepezil dosing participated in two task-related fMRI sessions consisting of a face-name paired associative encoding memory paradigm 24 weeks apart during a randomized placebo-controlled pharmaco-fMRI drug study." | ( Tracking cognitive change over 24 weeks with longitudinal functional magnetic resonance imaging in Alzheimer's disease. Atri, A; Deluca, AN; Diamond, EL; McLaren, DG; Mitchell, MB; O'Brien, JL; Rentz, DM; Sperling, RA; Sreenivasan, A; Van Dijk, KR, 2012) | 0.75 |
| " Previous nonclinical reports supporting oral dosing have utilized liquid chromatography tandem mass spectrometry (LC/MS/MS) to quantify donepezil concentrations in plasma." | ( Dried blood spot analysis of donepezil in support of a GLP 3-month dose-range finding study in rats. Arjmand, FM; Diehl, L; Huang, B; Lucke, RM; Meier-Davis, SR; Meng, M; Nagata, T; Shudo, J; Wen, J; Yuan, W, ) | 0.63 |
| "The purpose of this study was to develop an injectable depot liposphere delivery system with high loading capacity for controlled delivery of donepezil to decrease dosing frequency and increase patient compliance." | ( Biodegradable donepezil lipospheres for depot injection: optimization and in-vivo evaluation. Elsayed, I; Elshafeey, AH; Yehia, SA, 2012) | 0.94 |
| " Mini-Mental State Examination and Alzheimer's Disease Assessment Scale (ADAS) scores were determined before and after the donepezil dosage increase." | ( Efficacy of a high dosage of donepezil for Alzheimer's disease as examined by single-photon emission computed tomography imaging. Abe, S; Fujii, H; Iwamoto, T; Kanaya, K; Koizumi, K; Sakai, M, 2012) | 0.88 |
| "After the donepezil dosage increase, adverse effects associated with gastrointestinal symptoms were observed in one patient, and irritability was observed in three." | ( Efficacy of a high dosage of donepezil for Alzheimer's disease as examined by single-photon emission computed tomography imaging. Abe, S; Fujii, H; Iwamoto, T; Kanaya, K; Koizumi, K; Sakai, M, 2012) | 1.07 |
| "Increasing the donepezil dosage from 5 mg/day to 10 mg/day is effective for the treatment of AD." | ( Efficacy of a high dosage of donepezil for Alzheimer's disease as examined by single-photon emission computed tomography imaging. Abe, S; Fujii, H; Iwamoto, T; Kanaya, K; Koizumi, K; Sakai, M, 2012) | 1.02 |
| " While longer randomized controlled trials, increase dosage and selected groups of patients at different stage of cognitive impairment may provide a better understanding of the potential for this drug in addressing cognitive deficits, results to date have not been encouraging." | ( Assessing the prospect of donepezil in improving cognitive impairment in patients with schizophrenia. Henderson, DC; Thakurathi, N; Vincenzi, B, 2013) | 0.69 |
| "4 μM, while in other cells it augmented the current with a bell-shaped dose-response curve." | ( Donepezil in low micromolar concentrations modulates voltage-gated potassium currents in pyramidal neurons of rat hippocampus. Bukanova, JV; Skrebitsky, VG; Solntseva, EI, 2013) | 1.83 |
| " Demographic variables, quantity and rate of prescriptions, dosage forms and strengths were analyzed." | ( [Drugs used for cognitive impairment. Analysis of 1.5 million prescriptions in Argentina]. Arizaga, RL; Demey, I; Rojas, G, 2013) | 0.39 |
| " (clinical periods, late donepezil treatment) with the dosage of 1, 2 and 4 mg/kg/d respectively and the treatments persisted throughout the experiments." | ( The anti-inflammatory effect of donepezil on experimental autoimmune encephalomyelitis in C57 BL/6 mice. Chen, S; Chen, X; Jiang, Y; Kang, Z; Liu, M; Liu, Y; Ma, L; Ma, X; Peng, F; Pi, R; Wang, Q; Wu, A; Zhu, C; Zhu, D; Zou, Y, 2013) | 0.98 |
| "Because cognitive function showed improvement after increasing the dose of donepezil, the dosage of this drug should probably be adjusted based on the overall severity of Alzheimer's disease as well as the progression of cognitive dysfunction." | ( Efficacy of increasing donepezil in mild to moderate Alzheimer's disease patients who show a diminished response to 5 mg donepezil: a preliminary study. Hashimoto, M; Honda, K; Ikeda, M; Kaneda, K; Ogawa, Y; Yatabe, Y; Yuuki, S, 2013) | 0.93 |
| " In case of orally disintegrating tablet (ODT) containing bitter medicine, in vitro and in vivo disintegration is also importance for dosage performance." | ( In vitro and in vivo correlation of disintegration and bitter taste masking using orally disintegrating tablet containing ion exchange resin-drug complex. Cao, QR; Cho, SM; Cui, JH; Kim, JI; Lee, BJ; Oh, E, 2013) | 0.39 |
| " The Food and Drug Administration's recent approval of the increased dosage strength, donepezil 23 mg, previously only available in 5 mg and 10 mg strengths, has raised efficacy and safety concerns." | ( Donepezil 23 mg: a brief insight on efficacy and safety concerns. Nguyen, MD; Salbu, RL, 2013) | 2.06 |
| " RO by donepezil was calculated from a modified Lassen plot, and ED50 was estimated from the sigmoidal dose-response curves obtained when the RO was plotted against log donepezil dose." | ( Dose-dependent sigma-1 receptor occupancy by donepezil in rat brain can be assessed with (11)C-SA4503 and microPET. Dierckx, RA; Elsinga, PH; Ishiwata, K; Luurtsema, G; Nyakas, CJ; Ramakrishnan, NK; Schepers, M; van Waarde, A; Visser, AK, 2014) | 1.12 |
| " Donepezil dosage was then increased to 10 mg/day for 12 weeks." | ( Effects of donepezil dose escalation in Parkinson's patients with dementia receiving long-term donepezil treatment: an exploratory study. Hattori, N; Ishikawa, K; Kubo, S; Mizuno, Y; Motoi, Y, 2014) | 1.7 |
| "Inclusion criteria were double-blind, placebo-controlled trials of any length comparing patients diagnosed with probable Alzheimer disease (according to the NINCDS-ADRDA/DSM-III/IV criteria) taking any dosage of donepezil." | ( The effect of funding sources on donepezil randomised controlled trial outcome: a meta-analysis. Abrahams, S; Della Sala, S; Killin, LO; Russ, TC; Starr, JM, 2014) | 0.87 |
| "The present results suggest that a clinical dosage of DPZ accelerates angiomyogenesis by directly acting on both endothelial and satellite cells." | ( Donepezil can improve ischemic muscle atrophy by activating angiomyogenic properties of satellite cells. Arikawa, M; Doi, Y; Hoshino, E; Iiyama, T; Kakinuma, Y; Kitaoka, H; Kubo, T; Noguchi, T; Okazaki, K; Sato, T, 2014) | 1.85 |
| " The present research work pertains to the preparation of transdermal patches of donepezil with the objective to improve its patient compliance, therapeutic efficacy and to reduce the frequency of dosing and side effects as well as to avoid its extensive first pass metabolism." | ( Formulation and evaluation of transdermal patches of donepezil. Argade, NS; Dua, K; Madan, JR, 2015) | 0.89 |
| " The rationale for the higher dose formulation was the expected increase in acetylcholinesterase inhibition given the dose-response relationship of donepezil, with the benefits of the higher dose being most apparent in patients with more advanced AD." | ( Donepezil across the spectrum of Alzheimer's disease: dose optimization and clinical relevance. Dash, A; Jeong, SK; Kim, BC; Lee, JH; Park, KW, 2015) | 2.06 |
| " We also studied the optimal dosage regimen with repeated patch application for achieving a therapeutic range using a PK simulation model." | ( Therapeutic dosage assessment based on population pharmacokinetics of a novel single-dose transdermal donepezil patch in healthy volunteers. Bae, KS; Choi, HY; Hong, D; Kim, SS; Kim, YH; Lim, HS, 2015) | 0.63 |
| "Combining two standard-of-care medications for Alzheimer's disease (AD) into a single once-daily dosage unit may improve treatment adherence, facilitate drug administration, and reduce caregiver burden." | ( A novel once-daily fixed-dose combination of memantine extended release and donepezil for the treatment of moderate to severe Alzheimer's disease: two phase I studies in healthy volunteers. Boinpally, R; Chen, L; Hofbauer, RK; McClure, N; Periclou, A; Zukin, SR, 2015) | 0.65 |
| " Therefore, increasing the dosage of donepezil is a safe and effective treatment for patients with DLB who experience a relapse of BPSD." | ( Increased dosage of donepezil for the management of behavioural and psychological symptoms of dementia in dementia with Lewy bodies. Ino, T; Kosaka, K; Manabe, Y; Yamanaka, K, 2016) | 1.03 |
| " Considering that a 10 mg/day dose is approved for SAD in Japan, the present findings suggest that IR 10 mg/day donepezil is the optimal dosage for Japanese patients with SAD." | ( Efficacy and Safety of Sustained Release Donepezil High Dose versus Immediate Release Donepezil Standard Dose in Japanese Patients with Severe Alzheimer's Disease: A Randomized, Double-Blind Trial. Atarashi, H; Homma, A; Kubota, N; Nakai, K; Takase, T, 2016) | 0.91 |
| "Our results suggest that the developed formulation has a potential to replace the current daily dosing regimen to a less frequent dosing schedule." | ( Long Acting Ionically Paired Embonate Based Nanocrystals of Donepezil for the Treatment of Alzheimer's Disease: a Proof of Concept Study. Arya, A; Banala, VT; Mishra, PR; Mishra, S; Mitra, K; Mittapelly, N; Pandey, G; Sharma, S; Shukla, S; Thalla, M, 2017) | 0.7 |
| " However, a dose-response study evaluating DON after a controlled cortical impact (CCI) injury in rats did not reveal cognitive benefits." | ( Systemic administration of donepezil attenuates the efficacy of environmental enrichment on neurobehavioral outcome after experimental traumatic brain injury. Bondi, CO; Bou-Abboud, CE; Cheng, JP; Day-Cooney, J; Folweiler, KA; Kline, AE; Leary, JB; Memarzadeh, K; Tehranian-DePasquale, R; Yelleswarapu, NK, 2018) | 0.78 |
| " The method applied for biowaiver study of Donepezil Hydrochloride (DH) as a representative model was done by comparing two different dosage forms containing 5mg DH per tablet as an application of a developed chemometric method for correcting interferences as well as for the assay and dissolution testing in its tablet dosage form." | ( Chemometrics-assisted spectrophotometric green method for correcting interferences in biowaiver studies: Application to assay and dissolution profiling study of donepezil hydrochloride tablets. Elmallah, OA; Haggag, RS; Korany, MA; Mahgoub, H; Ragab, MAA, 2018) | 0.94 |
| " However, more patients treated with high dosage of donepezil discontinued their treatment due to various adverse events (AEs)." | ( A review of clinical treatment considerations of donepezil in severe Alzheimer's disease. Adlimoghaddam, A; Albensi, BC; Neuendorff, M; Roy, B, 2018) | 0.99 |
| " Current study concludes prepared Hyperbranched cellulose nanofiber will be good alternative for commercially available dosage forms for the treatment of Alzheimer's diseases." | ( Hyperbranched cellulose polyester of oral thin film and nanofiber for rapid release of donepezil; preparation and in vivo evaluation. AnjiReddy, K; Karpagam, S, 2019) | 0.74 |
| " Among all AChEIs donepezil possesses lowest adverse effects, it can treat mildmoderate- severe AD and only once-daily dosing is required." | ( De-novo Drug Design, Molecular Docking and In-Silico Molecular Prediction of AChEI Analogues through CADD Approaches as Anti-Alzheimer's Agents. Pandey, S; Singh, BK, 2020) | 0.89 |
| " To evaluate the protocol, brain sections from mice dosed intraperitoneally with donepezil, tacrine, clozapine, haloperidol, and aripiprazole were used." | ( Development of an Integrated Tissue Pretreatment Protocol for Enhanced MALDI MS Imaging of Drug Distribution in the Brain. Chen, Y; Gordon, A; Li, B; Tang, W, 2020) | 0.78 |
| "0 mA of intensity), and the needles were kept for 40 min, EA was given once a day; the donepezil hydrochloride tablet was taken orally, 5 mg, once a day, and after 4 weeks the dosage might be increased to 10 mg per day according to the specific situation." | ( [Effect of electroacupuncture at governor vessel on learning-memory ability and serum level of APP, Aβ Li, HL; Li, SL; Pang, J; Wang, YJ; Xia, KP; Zhang, M, 2020) | 0.78 |
| " There are few medications available as oral and suspension dosage forms for the management of AD." | ( Treatment of Alzheimer's diseases using donepezil nanoemulsion: an intranasal approach. Awasthy, S; Bhatnagar, I; Dang, S; Kaur, A; Nigam, K; Shankar, S; Sukhpal, H; Tyagi, A, 2020) | 0.83 |
| "This study characterized the pharmacokinetics (PKs) of a donepezil patch formulation currently under development, using mixed effect modeling analysis, and explored optimal patch dosing regimens in comparison with the donepezil oral formulation." | ( Pharmacokinetic Evaluation by Modeling and Simulation Analysis of a Donepezil Patch Formulation in Healthy Male Volunteers. Bae, KS; Choi, YK; Hong, DH; Kim, SS; Lim, HS; Yoon, SK, 2020) | 1.04 |
| " The relative bioavailability (BA) of donepezil after the patch application compared with oral dosing was described to be affected by the duration of patch application." | ( Pharmacokinetic Evaluation by Modeling and Simulation Analysis of a Donepezil Patch Formulation in Healthy Male Volunteers. Bae, KS; Choi, YK; Hong, DH; Kim, SS; Lim, HS; Yoon, SK, 2020) | 1.06 |
| " Medical charts were reviewed, including diagnosis, dosage of antidementia medicines, neuropsychological testing scores, and the further questionnaires were conducted via face-to-face or telephone, included duration of treatment, types of antidementia drugs, and reasons for treatment discontinuation." | ( Usage and adherence of antidementia drugs in a memory clinic cohort in Chongqing, Southwest China. Lü, Y; Yang, W; Yu, W; Yu, X, 2020) | 0.56 |
| " Besides, transdermal drug delivery systems seem to provide hope for the management of various diseases, due to the advantages that they offer in comparison with oral dosage forms." | ( Transdermal Drug Delivery Systems and their Potential in Alzheimer's Disease Management. Bülbül, EÖ; Karantas, ID; Mutlu, G; Okur, ME; Okur, NÜ; Siafaka, PI, 2020) | 0.56 |
| " These data support a novel antidepressant-like role for donepezil at lower doses as part of an overall u-shaped dose-response curve." | ( The cholinesterase inhibitor donepezil has antidepressant-like properties in the mouse forced swim test. Fitzgerald, PJ; Ghimire, A; Hale, PJ; Watson, BO, 2020) | 1.09 |
| " 3xTg-AD mice (10-month-old) were dosed intraperitoneally with 9R (daily 3, 10 or 30 mg/kg) for a month." | ( 9R, the cholinesterase and amyloid beta aggregation dual inhibitor, as a multifunctional agent to improve cognitive deficit and neuropathology in the triple-transgenic Alzheimer's disease mouse model. Ju, Y; Tam, KY, 2020) | 0.56 |
| " Donepezil (3 mg/kg; po) and sertraline (10 mg/kg; po) dosing was started from D-8 and continued up to D-32." | ( Development and treatment of cognitive inflexibility in sub-chronic stress-re-stress (SRS) model of PTSD. Krishnamurthy, S; Prajapati, SK, 2021) | 1.53 |
| " There was no significant association between age or the dosage of donepezil and the likelihood of reporting bradycardia." | ( Bradycardia Due to Donepezil in Adults: Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Eckhoff, K; Jose, RP; Luboff, H; Morris, R; Pham, M; Rohlsen-Neal, D, 2021) | 1.19 |
| "0 mg/kg), donepezil tended to promote depression-like behavior, suggesting a u-shaped dose-response curve for FST immobility." | ( Multiple cholinesterase inhibitors have antidepressant-like properties in the mouse forced swim test. Fitzgerald, PJ; Ghimire, A; Hale, PJ; Watson, BO, 2021) | 1.02 |
| " For AD patients, the dosage regimen is also crucial due to aging and diseases." | ( An Update on the Routes for the Delivery of Donepezil. Chen, BZ; Guo, XD; Zhang, XP; Zhao, ZQ; Zheng, H, 2021) | 0.88 |
| "Novel formulations of donepezil (DNP)-loaded microspheres based on a bio-degradable polymer of poly(lactic-co-glycolic acid) (PLGA) with a one-month duration of effect were developed, aimed at reducing dosing frequency and adverse effects and improving patient adherence." | ( Long-acting injectable donepezil microspheres: Formulation development and evaluation. Cho, HY; Choi, GW; Kang, DW; Kim, JH; Lee, S, 2021) | 1.25 |
| " Given the limitations of a smaller sample size, variables such as severity of disease, renal and liver impairment as well as medication dosing were not significant predictors (Table 3) for those reporting side effects on combination therapy." | ( Tolerability of memantine monotherapy versus adding memantine as combination therapy. Isaac, E; Keith, S; Lippa, C; Ney, D; Serruya, M; Sperling, MR, 2022) | 0.72 |
| " Improvements to the approved therapies, such as easier routes of administration and reduced dosing frequencies, along with the developments of new strategies and combined treatments are expected to occur within the next decade and will positively impact the way the disease is managed." | ( Symptomatic and Disease-Modifying Therapy Pipeline for Alzheimer's Disease: Towards a Personalized Polypharmacology Patient-Centered Approach. Boada, M; Jofresa, S; Morató, X; Pytel, V; Ruiz, A, 2022) | 0.72 |
| " However, the appropriate donepezil dosage is still a matter of debate." | ( The measured CSF/plasma donepezil concentration ratio but not individually measured CSF and plasma concentrations significantly increase over 24 h after donepezil treatment in patients with Alzheimer's disease. Angelucci, F; Dlabkova, A; Hort, J; Karasova, JZ; Kuca, K; Novotny, M; Pavelek, Z; Pejchal, J; Valis, M, 2023) | 1.52 |
| "In this study, donepezil-loaded PLGA and PLA microspheres (Dp-PLGA-M/Dp-PLA-M) and Dp-PLA-M wrapped in a polyethylene glycol-b-polycaprolactone (PC) hydrogel (Dp-PLA-M/PC) were prepared to reduce the dosing frequency of injections to treat Alzheimer's disease patients." | ( Preparation and evaluation of injectable microsphere formulation for longer sustained release of donepezil. Choi, S; Ji, YB; Ju, HJ; Kim, HE; Kim, MS; Lee, HB; Lee, S; Noh, JH; Park, K, 2023) | 1.48 |
| "This work focuses on developing nanoemulsions using a low-energy emulsification method for the codelivery of donepezil and memantine in one dosage form intended to be administered via the intranasal route for enhanced brain delivery." | ( Simultaneous Intranasal Codelivery of Donepezil and Memantine in a Nanocolloidal Carrier: Optimization, Pharmacokinetics, and Pharmacodynamics Studies. Bhatta, RS; Handa, M; Palkhade, R; Patil, GP; Sanap, SN; Shukla, R; Singh, DP, 2023) | 1.39 |
| "The current work is focused on developing mannose-coated PLGA nanoparticles for delivering Donepezil and Memantine in one dosage form." | ( Combining donepezil and memantine via mannosylated PLGA nanoparticles for intranasal delivery: Characterization and preclinical studies. Bhatta, RS; Ghose, S; Handa, M; Patil, GP; Sanap, SN; Shukla, R; Singh, DP, 2023) | 1.53 |
| Role | Description |
|---|---|
| EC 3.1.1.7 (acetylcholinesterase) inhibitor | An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of enzyme acetylcholinesterase (EC 3.1.1.7), which helps breaking down of acetylcholine into choline and acetic acid. |
| nootropic agent | Any compound that improves mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. |
| EC 3.1.1.8 (cholinesterase) inhibitor | An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of cholinesterase (EC 3.1.1.8). |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| racemate | A racemate is an equimolar mixture of a pair of enantiomers. |
| indanones | |
| piperidines | |
| aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| Integrated breast cancer pathway | 98 | 18 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 6.3096 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| geminin | Homo sapiens (human) | Potency | 37.5857 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 10.1815 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Acetylcholinesterase | Homo sapiens (human) | EC50 (µMol) | 0.0430 | 0.0190 | 0.5755 | 1.1400 | AID73711 |
| Acetylcholinesterase | Homo sapiens (human) | Kd | 0.0080 | 0.0080 | 1.7750 | 5.3000 | AID1756683 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1552606 | In vivo antioxidant activity in albino mouse assessed as increase in scopolamine-induced catalase activity by measuring decrease in H2O2 level in brain at 5 mg/kg, po administered once daily for 7 days followed by scopolamine challenge | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1537666 | Neuroprotective activity against H2O2-induced cytotoxicity in human SH-SY5Y cells assessed as cell viability at 10 uM preincubated for 3 hrs followed by H2O2 addition and measured after 24 hrs by MTT assay (Rvb = 75.2 +/- 4.6%) | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID289396 | Inhibition of Electrophorus electricus AchE-induced beta amyloid protein 1-42 co-aggregation at 100 uM by thioflavin T assay | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | 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. |
| AID1201378 | Half life in Sprague-Dawley rat liver microsomes at 2 uM at pH 7.4 pre-incubated in presence of NADPH regenerating system measured 30 mins after microsomal reactions termination by LC-MS method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Blood-brain barrier permeable anticholinesterase aurones: synthesis, structure-activity relationship, and drug-like properties. |
| AID1400277 | Inhibition of electric eel AChE-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by thioflavin-T fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
| AID1569988 | Inhibition of self-induced aggregation of amyloid beta (1 to 42) (unknown origin) at 25 uM incubated for 24 hrs by thioflavin-T fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1820983 | Anti-neuroinflammation in mouse BV-2 cells assessed as decrease in LPS-induced TNF-alpha production at 1.25 umol/L measured after 24 hrs by ELISA | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1321428 | Cognitive enhancing effect in ip dosed rat assessed as increase in recognition index treated 30 mins prior test measured after 24 hrs by novel object recognition test relative to vehicle-treated control | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19 | Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1378881 | Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1503620 | Inhibition of AChE (unknown origin) at 500 nM pre-incubated for 20 mins before acetylthiocholine iodide substrate addition by Ellman reagent based spectrophotometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease. |
| AID1707763 | Reversible inhibition of recombinant human BChE assessed as residual activity at 0.1 times IC50 using butyrylthiocholine iodide as substrate preincubated for 30 mins followed by 100-fold dilution in presence of substrate and measured after 15 mins by Ellm | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1635490 | Neuroprotective activity against H2O2-induced oxidative damage in human SH-SY5Y cells assessed as increase in cell viability at 10 uM incubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1261787 | Cognitive enhancing effect in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as reduction in searching distance at 2 mg/kg/day administered as intragastric infusion for 32 days measured during compound dosing by Morris water maze assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1335243 | Inhibition of human recombinant AChE preincubated for 5 mins followed by acetylthiocholine iodide substrate addition measured after 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT |
| AID1633169 | Selectivity index, ratio of IC50 for inhibition of human serum butyrylcholinesterase to IC50 for inhibition of human erythrocyte acetylcholinesterase | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1633184 | Reversal of scopolamine-induced spatial memory impairment in Wistar rat model of amnesia assessed as increase in spontaneous alteration at 5 mg/kg, po administered once daily for 1 week followed by scopolamine challenge 30 mins prior to test by Y-maze tes | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1478775 | Inhibition of equine serum BuChE using s-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 sec by Ellman's method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. |
| AID1201558 | Antiamnesic activity in NMRI mouse assessed as reversal of scopolamine-induced spontaneous alteration deficit at 1 mg/kg, ip by Y maze test | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Novel multitarget-directed ligands (MTDLs) with acetylcholinesterase (AChE) inhibitory and serotonergic subtype 4 receptor (5-HT4R) agonist activities as potential agents against Alzheimer's disease: the design of donecopride. |
| AID1201381 | Stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining at 2 uM measured 30 mins after microsomal reactions termination at pH 7.4 pre-incubated in presence of NADPH regenerating system by LC-MS method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Blood-brain barrier permeable anticholinesterase aurones: synthesis, structure-activity relationship, and drug-like properties. |
| AID748747 | Antiamnesic activity in Charles Foster albino rat assessed as reduction in scopolamine-induced increase in transfer latency at 5 mg/kg, po administered for 8 days measured 30 mins post last dose by elevated plus maze task (Rvb = 62.50 +/- 0.76 s) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Design, synthesis and evaluation of some new 4-aminopyridine derivatives in learning and memory. |
| AID1673642 | Displacement of propidium iodide from PAS region of human erythrocytes AChE at 50 uM incubated for 6 hrs by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1308844 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at > 30 times IC50 for AchE after 48 hrs by MTT assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1888435 | Inhibition of NO production in LPS-induced mouse BV-2 cells pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID781329 | pKa (acid-base dissociation constant) as determined by other workers | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID1709526 | Anti-VaD activity against BCCAO-induced Sprague-Dawley rat model of spatial memory deficit assessed as improvement in spatial learning and memory by measuring increase in number of neurons at 1 mg/kg, ig administered for 2 weeks followed by surgery and su | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Twin drug design, synthesis and evaluation of diosgenin derivatives as multitargeted agents for the treatment of vascular dementia. |
| AID314091 | Inhibition of human AchE | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Multi-target-directed ligands to combat neurodegenerative diseases. |
| AID1368603 | Inhibition of AchE in brain homogenates of scopolamine-induced albino mouse memory deficit model at 10 uM using acetylthiocholine iodide as substrate incubated for 10 mins measured for 2 mins by Ellman's method relative to control | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1335239 | Inhibition of equine serum BuChE preincubated for 5 mins followed by butyrylthiocholine iodide substrate addition measured after 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT |
| AID1773283 | Anti-alzheimer activity against scopolamine-induced cognitive dysfunction mouse model assessed as increase in number of platform crossing at 10 mg/kg, ip measured after 60 mins by Morris water maze test | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1867628 | Inhibition of human recombinant FAAH using AMC-AA as substrate preincubated with enzyme for 10 mins followed by substrate addition for 2 hrs by fluorometric analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease. |
| AID1854696 | Inhibition of Electrophorus electricus AchE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric based Ellman's method | 2022 | Bioorganic & medicinal chemistry, 10-01, Volume: 71 | Synthesis and biological evaluation of 4-hydroxy-methylpiperidinyl-N-benzyl-acylarylhydrazone hybrids designed as novel multifunctional drug candidates for Alzheimer's disease. |
| AID1879286 | Inhibition of BuchE (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 61 | 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. |
| AID395658 | Inhibition of BChE in rat serum after 15 mins by modified Ellman method | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives. |
| AID1472427 | Drug uptake in Wistar Han rat brain at 10 mg/kg, ip after 1 hr by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity. |
| AID1230942 | Inhibition of human recombinant AChE by spectrophotometric Ellman's method | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14 | Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases. |
| AID1338169 | Inhibition of BuChE (unknown origin) at 5 uM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease. |
| AID771356 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 2 mins by Ellman's method | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Design, synthesis, biological evaluation and docking study of 5-oxo-4,5-dihydropyrano[3,2-c]chromene derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID1162590 | Inhibition of human recombinant BuChE using butyrylthiocholine iodide substrate incubated for 15 mins by spectrophotometry based Ellman's method | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | 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. |
| AID1736966 | Reversible inhibition of human BChE assessed as residual activity at IC50 concentration relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1711764 | Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity preincubated for 15 mins followed by AAPH addition and measured every minute for 80 mins by ORAC-FL assay | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Development of cyanopyridine-triazine hybrids as lead multitarget anti-Alzheimer agents. |
| AID1445557 | Antioxidant activity assessed as DPPH free radical scavenging after 40 mins incubation in dark | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a "Bio-Oxidizable" Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation. |
| AID1480844 | Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity at 1 uM pretreated for 15 mins followed by APPH challenge measured every minute for 240 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1756681 | Inhibition of rat cortex homogenate acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1666047 | Reduction in the Abeta(1-42) peptide level in ICR mouse model of Abeta(1-42)-induced cognition-impairment at 15 mg/kg, po dosed from days 3 to 14 by ELISA relative to control | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor. |
| AID31627 | Inhibition against Acetylcholinesterase (AChE) | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | A comparative molecular field analysis study of N-benzylpiperidines as acetylcholinesterase inhibitors. |
| AID1465303 | Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1591465 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel Ache | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Naphthalene-triazolopyrimidine hybrid compounds as potential multifunctional anti-Alzheimer's agents. |
| AID1609197 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured for 1 min by DTNB reagent-based spectrophotometric analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1698422 | Inhibition of human AChE-induced amyloid beta (1 to 42) aggregation assessed as normalized fluorescence intensity at 5 to 20 uM by thioflavin T-based fluorometric assay relative to control | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1368596 | Inhibition of AchE in albino LACA mouse brain using acetylthiocholine iodide as substrate incubated for 10 mins measured for 2 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1693558 | Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate incubated for 10 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID1703582 | Permeability of the compound at pH 7.4 measured after 6 hrs by PAMPA method | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Discovery of novel berberine derivatives with balanced cholinesterase and prolyl oligopeptidase inhibition profile. |
| AID1884573 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 10 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID1635484 | Inhibition of equine serum BuChE using BTCI as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID725912 | Selectivity ratio of IC50 for BuChE in Sprague-Dawley rat serum to IC50 for AChE in Sprague-Dawley rat cortices | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors. |
| AID763840 | Cognitive enhancing effect in Charles Foster rat assessed as reversal of scopolamine-induced amnesia measured as transfer latency at 5 mg/kg, po for 8 days administered 1 hr prior to scopolamine-challenge on day 7 measured on day 8 by elevated plus maze t | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1657137 | Inhibition of Electrophorus electricus AChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method | 2020 | Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8 | Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. |
| AID1596489 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | A multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer's disease. |
| AID1552599 | Antialzheimer activity in albino mouse assessed as reversal of scopolamine-induced AChE level in brain at 5 mg/kg, po administered once daily for 7 days followed by scopolamine challenge using acetylthiocholine iodide as substrate by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1594061 | Inhibition of mouse brain homogenate AChE using acetylthiocholine iodide as substrate measured after 15 mins in presence of BChE inhibitor methopropazine hydrochloride by DTNB reagent based colorimetric method | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13 | A new lateral root growth inhibitor from the sponge-derived fungus Aspergillus sp. LS45. |
| AID1225714 | Reversal of scopolamine-induced cognitive deficit in Kunming mouse assessed as latency time at 0.5 mg/kg, po administered 1 hr before training trial measured at 24 hrs after training trial by passive avoidance test | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1201371 | Inhibition of electric eel AChE incubated for 15 mins using acetylcholine iodide substrate by colorimetric Ellman's method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Blood-brain barrier permeable anticholinesterase aurones: synthesis, structure-activity relationship, and drug-like properties. |
| AID1389179 | Inhibition of electric eel AChE at 10 uM using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease. |
| AID1888441 | Inhibition of amyloid beta (1 to 42 ) (unknown origin) self aggregation at 100 uM measured after 48 hrs by thioflavin-T fluorescence method relative to control | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1225701 | Inhibition of self-induced Abeta(1 to 42) (unknown origin) aggregation at 25 uM after 24 hrs by Thioflavin T-based fluorometric assay | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1732084 | Inhibition of BuChE in human serum using butyrylthiocholineiodide as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by DTNB reagent based Ellman's method | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | 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. |
| AID1772614 | Inhibition of electric eel recombinant AChE preincubated for 1 min in presence of DNTB followed by addition of acetylthiocholine iodide substrate and measured after 20 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID1193153 | Inhibition of BuChE in horse serum pre-incubated for 5 mins before addition of butyrylthiocholine iodide substrate by Ellman's assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents. |
| AID1705718 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every minute for 10 mins by DTNB-reagent based Ellman's method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase. |
| AID1762615 | Neuroprotection against icv infused amyloid beta (1 to 42)-induced ICR mouse model of Alzheimer's disease assessed as rescue of pyknotic nucleus in hippocampal at to 2 mg/kg, po administered daily for 7 days by HE staining | |||
| AID748771 | Inhibition of electric eel AChE using acetylcholine iodide as substrate incubated for 20 mins prior to substrate addition by Ellman method | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Design, synthesis and evaluation of some new 4-aminopyridine derivatives in learning and memory. |
| AID1303019 | Inhibition of AchE (unknown origin) | 2016 | ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4 | Stacking with No Planarity? |
| AID1261775 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as condensed cytoplasm in CA1 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxyl | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1125766 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 10 mins prior to substrate challenge measured after 15 mins by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Quinolone-benzylpiperidine derivatives as novel acetylcholinesterase inhibitor and antioxidant hybrids for Alzheimer disease. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID1486223 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate measured for 6 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis, docking study and neuroprotective effects of some novel pyrano[3,2-c]chromene derivatives bearing morpholine/phenylpiperazine moiety. |
| AID1459563 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1503619 | Inhibition of BuChE (unknown origin) at 500 nM pre-incubated for 20 mins before S-Butyrylthiocholine iodide substrate addition by Ellman reagent based spectrophotometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease. |
| AID1070082 | Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease. |
| AID1576113 | Neuroprotective activity against OGD-induced neurotoxicity in Sprague-Dawley rat cortical neuron assessed as cell survival rate at 1 uM pretreated for 24 hrs followed by incubation in oxygen and glucose deprivation medium for 2 hrs followed by exposure to | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | The synthesis and biological evaluation of novel gardenamide A derivatives as multifunctional neuroprotective agents. |
| AID1695784 | Selectivity index, ratio of inhibition of human erythrocyte AChE over inhibition of human serum BChE | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions. |
| AID1576114 | Neuroprotective activity against OGD-induced neurotoxicity in Sprague-Dawley rat cortical neuron assessed as cell survival rate at 10 uM pretreated for 24 hrs followed by incubation in oxygen and glucose deprivation medium for 2 hrs followed by exposure t | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | The synthesis and biological evaluation of novel gardenamide A derivatives as multifunctional neuroprotective agents. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1320878 | Antioxidant activity assessed as AAPH free radical scavenging activity by measuring trolox equivalent by oxygen radical absorbance capacity method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | 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. |
| AID31163 | Ex vivo inhibition of human erythrocyte Acetylcholinesterase. | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
| AID1784491 | Inhibition of human recombinant AChE using acetylthiocholine iodide as a substrate preincubated for 20 mins followed by substrate addition by spectrophotometric analysis | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | 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. |
| AID1517850 | Disaggregation of Cu2+ induced preformed fibrils of amyloid beta (1 to 42) at 25 uM preincubated with Cu2+ for 24 hrs followed by compound addition and measured after 24 hrs by thioflavin-T based fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1156824 | Selectivity ratio of IC50 for BuChE (unknown origin) to IC50 for AChE (unknown origin) | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | 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. |
| AID1533608 | Selectivity index, ratio of IC50 for human serum BChE to IC50 for Electric eel AChE | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1702421 | Selectivity index, ratio of IC50 for human serum BChe to IC50 for human erythrocytes AChE | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1217709 | Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1659411 | Inhibition of PDE5A (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease. |
| AID30826 | Inhibition of fetal Bovine serum AChE | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1 | Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors. |
| AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
| AID1076767 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 100 nM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rel | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1466563 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis | |||
| AID1609200 | Permeability of the compound in pH 7.4 PBS buffer incubated for 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1353362 | Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1245373 | Inhibition of equine serum BuChE using DTNB as substrate incubated for 5 mins prior to substrate addition measured after 2 mins by Ellman's method | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Multifunctional novel Diallyl disulfide (DADS) derivatives with β-amyloid-reducing, cholinergic, antioxidant and metal chelating properties for the treatment of Alzheimer's disease. |
| AID1167543 | Inhibition of human erythrocyte AChE preincubated for 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1220555 | Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
| AID1152914 | Inhibition of MAO-A in rat liver homogenate using [14C]-5HT as substrate preincubated for 30 mins followed by substrate addition measured after 20 mins by liquid scintillation counting analysis | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1682163 | Inhibition of rat cortex homogenate BuChE by spectrophotometric method | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1609222 | Improvement in learning and spatial memory in icv infused amyloid beta (1 to 42)-induced Wistar rat model of Alzheimer's disease assessed as increase in time spent in platform zone at 5 mg/kg, po administered daily for 7 days starting from 7 days post sur | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1736950 | Inhibition of human AChE-induced amyloid beta (1 to 40 residues) (unknown origin) aggregation at 100 uM by thioflavin-T fluorescence method relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID1484819 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1472437 | Inhibition of AChE in mouse brain homogenate using acetylthiocholine as substrate preincubated for 300 secs followed by substrate addition by Ellman's method | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity. |
| AID1498853 | Inhibition of self-induced human amyloid beta (1 to 42) aggregation at 25 uM after 24 hrs by thioflavin-T based fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Design, synthesis and evaluation of novel bivalent β-carboline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1709255 | Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1772615 | Inhibition of human recombinant N-terminal His-tagged GSK3beta expressed in Escherichia coli using RRRPASVPPSPSLS RHS(pS)HQRR as substrate incubated for 30 mins in presence of ATP by Kinase-Glo reagent based luminescence assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID1436055 | Inhibition of AChE in rat brain cortex homogenates using acetylthiocholine iodide as substrate in presence of BuChE inhibitor tetraisopropyl pyrophosphoramide measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease. |
| AID1569984 | Reversible inhibition of equine serum BuChE assessed as enzyme activity at 0.1xIC50 using butyrylthiocholine iodide as substrate measured after dilution by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1517859 | Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1635497 | Neuroprotective activity in Swiss albino mouse assessed as reduction in scopolamine-induced elevation in escape latency time at 5 mg/kg, po administered 30 mins prior to scopolamine challenge administered for 9 days measured for last 5 days of treatment b | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1764085 | Neuroprotective activity against rat PC12 cells under glucose and oxygen-deprived condition assessed as increase in cell viability at 1 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | The structural simplification of lysergic acid as a natural lead for synthesizing novel anti-Alzheimer agents. |
| AID1459561 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1673653 | Improvement in learning and spatial memory in icv infused amyloid beta (1 to 42)-induced rat model of Alzheimer's disease assessed as increase in number of platform crossing at 5 mg/kg, po administered daily for 7 days starting from 7 days post surgery an | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1707757 | Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1427510 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
| AID1866877 | Inhibition of equine serum BchE using S-butyryl thiocholine iodide as substrate incubated for 10 mins followed by substrate addition measured at 0 to 180 secs by Ellman's method | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors. |
| AID1335932 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-4 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1379010 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 180 secs by spectrophotometric analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1682335 | Inhibition of rat cortex homogenate acetylcholinesterase by spectrophotometric method | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID282008 | Inhibition of human recombinant BChE | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties. |
| AID1906403 | In vivo inhibition of AChE in ICR mouse cerebral cortex using acetylthiocholine iodide as substrate at 10 mg/kg, ig measured after 1 hr by microplate reader analysis | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID666575 | Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents. |
| AID1709524 | Toxicity in BCCAO-induced Sprague-Dawley rat model of spatial memory deficit assessed as effect on swimming speed at 1 mg/kg, ig administered for 2 weeks followed by surgery and subsequent compound dosing for 32 days by Morris water maze test | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Twin drug design, synthesis and evaluation of diosgenin derivatives as multitargeted agents for the treatment of vascular dementia. |
| AID1694881 | Inhibition of recombinant human MAO- A using p-tyramine as substrate preincubated with enzyme for 15 mins followed incubation with substrate for 20 mins by Amplex red reagent based fluorescence based analysis | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1347795 | Inhibition of amyloid beta (25 to 35 residues) (unknown origin)-induced toxicity in rat PC12 cells assessed as protection against amyloid beta (25 to 35 residues)-induced apoptosis by measuring late apoptotic cells at 50 ug/ml by Annexin V-FITC/propidium | |||
| AID1473876 | Ratio of drug concentration at steady state in human at 5 to 10 mg, po after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1406252 | Inhibition of BChE (unknown origin) | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities. |
| AID1906379 | Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of okadaic acid-induced mitochondrial dysfunction by measuring increase in red-to-green fluorescence intensity ratio pretreated for 24 hrs followed by okadaic acid addition for 24 hrs | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1201554 | Inhibition of propidium iodide binding to peripheral anionic site of electric eel AChE at 10 uM incubated for 6 hrs by propidium competition assay | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Novel multitarget-directed ligands (MTDLs) with acetylcholinesterase (AChE) inhibitory and serotonergic subtype 4 receptor (5-HT4R) agonist activities as potential agents against Alzheimer's disease: the design of donecopride. |
| AID1347796 | Inhibition of amyloid beta (25 to 35 residues) (unknown origin)-induced toxicity in rat PC12 cells assessed as protection against amyloid beta (25 to 35 residues)-induced apoptosis by measuring necrotic cells at 50 ug/ml by Annexin V-FITC/propidium iodide | |||
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1195138 | Effect on scopolamine-induced cognitive dysfunction in albino Swiss CD-1 mouse assessed as reduction in step-through latency time at 5 to 10 mg/kg, ip administered 1 hr before the acquisition trial by passive avoidance test | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with β-amyloid anti-aggregation properties and beneficial effects on memory in vivo. |
| AID1854698 | Selectivity ratio, ratio of IC50 for equine serum BuChE to IC50 for Electrophorus electricus AchE | 2022 | Bioorganic & medicinal chemistry, 10-01, Volume: 71 | Synthesis and biological evaluation of 4-hydroxy-methylpiperidinyl-N-benzyl-acylarylhydrazone hybrids designed as novel multifunctional drug candidates for Alzheimer's disease. |
| AID1378862 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1691665 | Inhibition of human serum BuChE assessed as residual activity at IC50 using acetylcholine iodide as substrate measured by Ellman's method relative to control | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1552589 | Selectivity index, ratio of IC50 for inhibition of human BChE to ratio of IC50 for inhibition of human AChE | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1569978 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1261781 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as pyknotic nucleus in CA3 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxylin | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1335938 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-9 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1581644 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate pre-incubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | 1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease. |
| AID1698411 | Inhibition of human AChE by Ellman's method | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1752607 | Displacement of propidium iodide from the PAS site of human AChE at 10 uM preincubated with enzyme for 6 hrs followed by incubation with propidium iodide and measured after 20 mins by fluorescence analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease. |
| AID1709254 | Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID31500 | Inhibitory concentration against acetylcholinesterase (AChE) from human erythrocytes | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | Aminopyridazines as acetylcholinesterase inhibitors. |
| AID1700052 | Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation incubated for 48 hrs by thioflavin-T fluorescence method | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation. |
| AID1762610 | Improvement in learning and spatial memory in icv infused amyloid beta (1 to 42)-induced ICR mouse model of Alzheimer's disease assessed as improved target quadrant exploration time at to 2 mg/kg, po administered daily for 7 days starting from 7 days post | |||
| AID241886 | In vitro inhibitory concentration against butyrylcholinesterase was determined using rat serum homogenate | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors. |
| AID695012 | Antialzheimer activity in Kunming mouse assessed as reversal of amyloid beta (1 to 42)-induced decrease of swimming time spent in target quadrant at 0.65 mg/kg, po qd measured on day 13 by morris water maze test | 2012 | ACS medicinal chemistry letters, Nov-08, Volume: 3, Issue:11 | Identification of aminopyridazine-derived antineuroinflammatory agents effective in an Alzheimer's mouse model. |
| AID1480936 | Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by UV-Vis spectrophotometric method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | 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. |
| AID1736967 | Reversible inhibition of human BChE assessed as residual activity at 0.1 times of IC50 concentration relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1655644 | Inhibition of human AChE using acetylthiocholineiodide as substrate measured for every 30 sec for 5 mins by Ellman's method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor. |
| AID1267380 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents. |
| AID1738115 | Disruption of human amyloid beta 1 to 42 assessed as effect on amyloid beta 1 to 42 morphology at 1.58 uM incubated for 10 days by atomic force microscopic analysis | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1444107 | Reversal of scopolamine-induced memory deficit in Kunming mouse assessed as step down latency time at 5 mg/kg, po treated for 1 hr before training followed by scopolamine challenge 30 mins before training measured 24 hrs after training trial by passive av | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1635493 | Antioxidant activity assessed as DPPH free radical scavenging activity at 20 uM after 30 secs by spectrophotometry | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1484826 | Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation at 25 uM after 24 hrs by ThT-based fluorometric method relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1311916 | Selectivity index, ratio of IC50 for equine BCHE to IC50 for electric eel ACHE | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1330786 | Hepatotoxicity in scopolamine-induced memory deficit Kunming mouse model assessed as distinct fatty degeneration in hepatocytes at 5 mg/Kg, po for 6 days by hematoxylin and eosin-staining based microscopic analysis | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1824587 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as intrinsic clearance measured upto 45 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1400286 | Reversal of scopolamine-induced memory impairment in albino Wistar rat assessed as decrease in mean training period traveled distance to find platform at 2.5 mg/kg, ip by Morris water maze test | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
| AID1167545 | Antioxidant activity assessed as oxygen radical absorbance capacity preincubated for 10 mins by fluorescence assay relative to trolox | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1816861 | Toxicity in ICR mouse assessed as increase in body weight administered for 14 days and measured daily | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection. |
| AID1290890 | Inhibition of self-induced amyloid beta (1 to 42) aggregation (unknown origin) at 25 uM after 24 hrs by thioflavin T fluorescence method | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease. |
| AID1555996 | Neuroprotective activity against H2O2 induced cytotoxicity in rat PC12 cells assessed as cell viability at 5 uM pretreated for 3 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay (Rvb = 35.69 to 50.26%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1784489 | Inhibition of human recombinant BACE-1 expressed in Escherichia coli using panvera peptide as a substrate incubated for 1 hr by fluorescence analysis | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | 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. |
| AID1217711 | Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1866875 | Antialzheimer activity in ICR mouse assessed as reduction in scopolamine-induced cognitive impairment, ip administered for 14 consecutive days followed by scopolmaine-stimulation measured on day 21 by Morris water maze test | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors. |
| AID31035 | Concentration required to inhibit 50% of Acetylcholinesterase obtained from human erythrocytes was determined in vitro | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors. |
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| AID1767559 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 10 uM measured after 48 hrs by MTT assay relative to control | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant. |
| AID588208 | Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset | 2010 | Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5 | Predicting phospholipidosis using machine learning. |
| AID1756683 | Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as dissociation constant at 298.15 K by surface plasmon resonance assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1739253 | Inhibition of AChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase. |
| AID1261723 | Half life in rat liver microsomes at 100 uM after 5 to 180 mins by HPLC-UV analysis | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1824590 | Inhibition of recombinant AChE in human erythrocytes using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1152934 | Hepatotoxicity in human HepG2 cells assessed as cell viability at 10 uM by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1339458 | Cognition enhancement activity in Charles Foster albino rat model of spatial working memory assessed as escape latency at 10 mg/kg, po for administered from day 1 to 10 measured 1 hr post last dose on day 9 by Morris water maze test (Rvb = 17.38 +/- 0.79 | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1498852 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BChE | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Design, synthesis and evaluation of novel bivalent β-carboline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1633171 | Displacement of Propidium iodide from PAS region of AChE (unknown origin) at 10 uM incubated for 6 hrs by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1351502 | Reversal of SCOP-induced cognitive impairment in Sprague-Dawley rat assessed as reduction in time spent exploring novel object over familiar object at 0.3 mg/kg, po administered 120 mins before familiarization phase measured for 3 mins post familiarizatio | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1695765 | Displacement of PI from human AChE PAS site at 30 uM preincubated for 6 hrs followed by PI addition and measured immediately by fluorescence assay relative to control | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions. |
| AID1824580 | Inhibition of BuChE in mouse serum using butyrylthiocholine iodide as substrate incubated for 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1545335 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID1707762 | Reversible inhibition of recombinant human AChE expressed in HEK293 cells assessed as residual activity at IC50 using acetylthiocholine iodide as substrate preincubated for 30 mins followed by 100-fold dilution in presence of substrate and measured after | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1397455 | Mixed-type inhibition of human recombinant AChE using 50 to 500 uM acetylthiocholine as substrate by Lineweaver-Burk plot analysis | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors. |
| AID404845 | Inhibition of rat cortex AChE | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1738334 | Inhibition of human plasma AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 10 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer's disease. |
| AID1506851 | Inhibition of AChE-induced amyloid beta (1 to 42 residues) (unknown origin) fibril formation at amyloid beta (1 to 42 residues)/AChE/compound ratio of 100:1:100 after 6 hrs by ThT-based fluorometric method relative to control | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Rational design, synthesis and biological screening of triazine-triazolopyrimidine hybrids as multitarget anti-Alzheimer agents. |
| AID1533623 | Ex vivo inhibition of AChE in Swiss albino mouse brain at 1 mg/kg, ip qd pretreated for 1 hr followed by scopolamine addition using acetylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1882051 | Selectivity ratio of IC50 for BuChE (unknown origin) to IC50 for AChE (unknown origin) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID1261755 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as irregular shape in CA2 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxylin a | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1707759 | Inhibition of electric eel AChE at 10 uM using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method relative to control | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID540235 | Phospholipidosis-negative literature compound | |||
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| AID1901723 | Ex vivo inhibition of AChE in Sprague-Dawley rat brain homogenate at 10 mg/kg, ip measured after 1 hr by ELISA relative to control | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents. |
| AID1406141 | Inhibition of human serum BuChE using butyrylthiocholine as substrate pretreated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease. |
| AID1308846 | Inhibition of horse serum BuChE using butyrylthiocoline iodide as substrate at 2 uM preincubated for 20 mins followed by 100 fold dilution by Ellman method | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1484818 | Antioxidant activity assessed as trolox equivalents of AAPH radical scavenging activity at 1 to 10 uM preincubated for 15 mins followed by AAPH addition measured every 60 sec for 90 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID289392 | Inhibition of human BChE by Ellman's method | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | 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. |
| AID1193154 | Selectivity index, ratio of IC50 for BuChE in horse serum to IC50 for Electrophorus electricus AChE | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents. |
| AID1698414 | Selectivity index, ratio of IC50 for human BChE to IC50 for human AChE by Ellman's method | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1353752 | Cytotoxicity against rat PC12 cells assessed as cell viability up to 50 uM after 24 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one scaffold derivatives: Synthesis and biological evaluation as selective BuChE inhibitors. |
| AID1570265 | Inhibition of human AChE at 100 uM using acetylthiocholine iodide as substrate after 10 secs measured at 30 s intervals for two minutes by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships. |
| AID1773262 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1152943 | Permeability in human Caco2 cells | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1444075 | Inhibition of BuChE in rat serum using butyrylthiocholine chloride as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1176151 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins at 0.1 uM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1824589 | Metabolic stability in CD-1 mouse liver microsomes assessed as intrinsic clearance measured upto 45 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1320875 | Inhibition of human recombinant MAOB using p-tyramine as substrate incubated for 15 mins by fluorimetric method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | 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. |
| AID1877960 | Antialzheimer activity against scopolamine-induced cognitive deficit mouse model assessed as increase in vitality of SOD at 5.0 mg/kg by step-through passive avoidance test | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease. |
| AID1542240 | Permeability of the compound at 30 to 50 uM at pH 7.4 measured up to 6 hrs by PAMPA-BBB assay method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| AID1738126 | Memory enhancement effect in scopolamine-induced Swiss albino mouse model of amnesia assessed as effect on total arm entries at 5 mg/kg, po administered for 7 days and observed after 30 mins before scopolamine treatment and measured after 15 mins by Y-maz | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1702435 | Inhibition of copper-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM by ThT fluorescence assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
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| AID1596167 | Inhibition of electric eel AChE assessed as inhibition constant using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by Dixon plot analysis | 2019 | European journal of medicinal chemistry, Jul-15, Volume: 174 | Benzoic acid-derived nitrones: A new class of potential acetylcholinesterase inhibitors and neuroprotective agents. |
| AID1191941 | Selectivity index, ratio of IC50 for rat serum BuChE to IC50 for AChE from rat cortex homogenate | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Design, synthesis and evaluation of chromone-2-carboxamido-alkylbenzylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1889346 | Reversible inhibition of human AChE assessed as enzyme recovery activity at 0.1 times of IC50 concentration by dilution method relative to control | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID469245 | Inhibition of Electrophorus electricus AChE by Ellman's method | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17 | Design, synthesis and evaluation of novel 5,6-dimethoxy-1-oxo-2,3-dihydro-1H-2-indenyl-3,4-substituted phenyl methanone analogues. |
| AID1633216 | Antiinflammatory activity in mouse BV2 cells assessed as reduction in LPS-induced TNF-alpha production at 10 uM pretreated for 1 hr followed by LPS challenge and measured after 24 hrs by ELISA assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1339445 | Ex vivo inhibition of AChE in Charles Foster albino rat brain assessed as substrate hydrolyzed per mg protein at 10 mg/kg, po measured after 1 hr using acetylthiocholine iodide as substrate by Ellman's method (Rvb = 46.56 +/- 0.66 nmol/min) | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1445547 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for AChE in human erythrocytes | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a "Bio-Oxidizable" Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation. |
| AID1317852 | Inhibition of electric eel AChE preincubated for 5 mins followed by addition of acetylthiocholine iodide as substrate measured after 2 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID345208 | Inhibition of self-induced amyloid beta (1-40) aggregation at 10 uM by thioflavin T formation assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer. |
| AID1772657 | Ex vivo inhibition of AChE in ICR mouse brain at 10 uM measured after 1 hr by Ellman method relative to control | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID1225690 | Inhibition of AChE in rat cortex using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID724168 | Inhibition of acetylcholinesterase (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase. |
| AID1853195 | Inhibition of human acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2022 | RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12 | Pyrazolines as potential anti-Alzheimer's agents: DFT, molecular docking, enzyme inhibition and pharmacokinetic studies. |
| AID1635488 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 40 uM after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1784492 | Inhibition of human serum BChE using butyrylthiocholine iodide as a substrate preincubated for 20 mins followed by substrate addition by spectrophotometric analysis | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | 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. |
| AID1367021 | Antialzheimer activity in Swiss albino mouse brain assessed as reversal of scopolamine-induced reduction in GSH levels at 2 mg/kg, ip (Rvb = 21.3 +/- 0.81) | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Exploration of multi-target potential of chromen-4-one based compounds in Alzheimer's disease: Design, synthesis and biological evaluations. |
| AID1738108 | Displacement of propidium iodide from human AChE at 10 uM incubated for 6 hrs followed by propidium iodide addition and measured after 20 mins by fluorescence based assay relative to control | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1176162 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 100 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1335931 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-3 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1815195 | Ratio of IC50 for cytotoxicity against human HepG2 cells to ratio of IC50 for inhibition of rat cortex AChE | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID1322903 | Inhibition of human recombinant MAOA using p-tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by horse-radish peroxidase/amplex red-based fluorometric method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation. |
| AID1633165 | Inhibition of human serum butyrylcholinesterase using BTCI as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1267381 | Inhibition of horse serum butyrylcholinesterase using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents. |
| AID1826352 | Inhibition of human recombinant MAO-B expressed in supersomes assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate by spectrofluorimetric analysis | |||
| AID1076177 | Selectivity ratio of IC50 for human recombinant MAO-B to IC50 for human recombinant MAO-A | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID44285 | Ex vivo inhibition of human plasma Butyrylcholinesterase. | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
| AID1501658 | Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by UV-Vis spectrophotometric analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID1379217 | Inhibition of amyloid beta (1 to 42) (unknown origin) self -induced aggregation at 10 uM after 48 hrs by ThT-based fluorescence method relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID1077090 | Inhibition of electric eel AchE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1166298 | Inhibition of human BChE by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Active compounds from a diverse library of triazolothiadiazole and triazolothiadiazine scaffolds: synthesis, crystal structure determination, cytotoxicity, cholinesterase inhibitory activity, and binding mode analysis. |
| AID1820950 | Reversible inhibition of electric eel AChE assessed as residual enzyme activity using acetylthiocholine iodide as substrate at 1 times IC50 incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1486222 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured for 6 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis, docking study and neuroprotective effects of some novel pyrano[3,2-c]chromene derivatives bearing morpholine/phenylpiperazine moiety. |
| AID1195134 | Inhibition of self-induced beta-amyloid (1 to 42) (unknown origin) at 10 uM aggregation by thioflavin-T assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with β-amyloid anti-aggregation properties and beneficial effects on memory in vivo. |
| AID1666044 | Improvement in cognition in ICR mouse model of Abeta(1-42)-induced cognition-impairment assessed as improvement in trajectories to platform at 15 mg/kg, po dosed from days 3 to 14 by Morris water maze test | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor. |
| AID1322904 | Inhibition of human recombinant MAOB using p-tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by horse-radish peroxidase/amplex red-based fluorometric method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation. |
| AID1576112 | Neuroprotective activity against OGD-induced neurotoxicity in Sprague-Dawley rat cortical neuron assessed as cell survival rate at 0.1 uM pretreated for 24 hrs followed by incubation in oxygen and glucose deprivation medium for 2 hrs followed by exposure | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | The synthesis and biological evaluation of novel gardenamide A derivatives as multifunctional neuroprotective agents. |
| AID1569989 | Inhibition of Cu2+ induced human amyloid beta (1 to 42) aggregation at 25 uM after 24 hrs by thioflavin-T fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1738105 | Inhibition of recombinant equine serum BuChE using butyryl thiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by spectrophotometry based Ellman's method | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1400273 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
| AID241692 | Inhibitory concentration against human erythrocyte Acetylcholinesterase | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine. |
| AID234643 | Selectivity at AChE and BChE | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
| AID1752598 | Inhibition of AChE in human erythrocytes using acetylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease. |
| AID707697 | Inhibition of mouse recombinant GST-tagged CLK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1626719 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 5 mins by spectrophotometric Ellman's method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Exploring Basic Tail Modifications of Coumarin-Based Dual Acetylcholinesterase-Monoamine Oxidase B Inhibitors: Identification of Water-Soluble, Brain-Permeant Neuroprotective Multitarget Agents. |
| AID1609219 | Improvement in learning and spatial memory in icv infused amyloid beta (1 to 42)-induced Wistar rat model of Alzheimer's disease assessed as reduction in escape latency at 5 mg/kg, po administered daily for 7 days starting from 7 days post surgery and mea | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID763843 | Non competitive inhibition of human serum BChE using butyrylthiocholine iodide as substrate by Lineweaver-Burk plot analysis | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1666043 | Improvement in cognition in ICR mouse model of Abeta(1-42)-induced cognition-impairment assessed as escape latency time at 15 mg/kg, po dosed from days 3 to 14 by Morris water maze test (Rvb = 48.9 secs) | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor. |
| AID595290 | Inhibition of human BChE using butyrylthiocholine iodide as substrate by Ellman's method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1503621 | Inhibition of BuChE (unknown origin) pre-incubated for 20 mins before S-Butyrylthiocholine iodide substrate addition by Ellman reagent based spectrophotometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease. |
| AID1736936 | Inhibition of electric eel AChE by Ellman's method | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1757184 | Inhibition of rat serum BuChE by Ellman's method | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease. |
| AID1176155 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins at 250 uM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1515405 | Toxicity against Artemia salina larvae assessed as larval mortality at 1000 ug/mL after 24 hrs relative to control | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2 | In silico, NMR and pharmacological evaluation of an hydroxyoxindole cholinesterase inhibitor. |
| AID1872733 | Inhibition of BChE (unknown origin) incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy. |
| AID1055218 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID1311921 | Selectivity index, ratio of IC50 for human serum BCHE to IC50 for human erythrocyte ACHE | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1703002 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by addition of substrate and measured after 20 mins by DTNB reagent based Ellman's method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | The structure-based optimization of δ-sultone-fused pyrazoles as selective BuChE inhibitors. |
| AID1824581 | Selectivity index,ratio of IC50 for inhibition of BuChE in mouse serum to IC50 for inhibition of AChE in mouse cortical homogenate | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1762427 | Inhibition of equine serum BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters. |
| AID1866913 | Antialzheimer activity in scopolamine-induced cognitive impairment ICR mouse model assessed as improvement of exploration ability, ip administered for 14 consecutive days followed by scopolmaine-stimulation measured on day 21 by Y maze test | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors. |
| AID657795 | Inhibition of mitochondrial MAO-B in rat liver homogenates using [14C]-phenylethylamine as substrate preincubated for 30 mins by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 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. |
| AID635813 | Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID1465277 | Inhibition of rat cortex homogenate AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | 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. |
| AID1309428 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Design, synthesis and evaluation of novel indandione derivatives as multifunctional agents with cholinesterase inhibition, anti-β-amyloid aggregation, antioxidant and neuroprotection properties against Alzheimer's disease. |
| AID1764086 | Neuroprotective activity against LPS-induced mouse SIM-A9 cells assessed as increase in cell viability at 1 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | The structural simplification of lysergic acid as a natural lead for synthesizing novel anti-Alzheimer agents. |
| AID1199520 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for Electrophorus electricus AChE | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID349883 | Inhibition of amyloid beta (1-42) self-aggregation at 50 uM after 24 hrs by thioflavin T fluorescence method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1368598 | Cognition enhancing effect in albino mouse assessed as reversal of scopolamine-induced memory deficit by measuring basal latency time at 0.5 mg/kg, ip treated 5 mins post scopolamine challenge by step down passive avoidance test (Rvb = 63.93 +/- 2.6 sec) | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1772661 | In vivo inhibition of AChE in ICR mouse brain assessed as acetycholine level at 10 mg/kg, po measured after 1.5 hrs by HPLC-MS/MS analysis relative to control | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID1625114 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities. |
| AID1773254 | Cytotoxicity against human HepG2 cells assessed as cell viability at 50 uM incubated for 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1591466 | Inhibition of electric eel Ache using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman method | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Naphthalene-triazolopyrimidine hybrid compounds as potential multifunctional anti-Alzheimer's agents. |
| AID1815196 | Inhibition of hERG expressed in CHO-K1 cells assessed as reduction in thallium influx incubated for 30 minutes by FLIPR | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID404846 | Inhibition of rat serum BChE | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1480854 | Inhibition of amyloid beta (1 to 42) (unknown origin) fibril formation at 20 uM measured up to 48 hrs by uranyl acetate staining based transmission electron microscopy | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID462782 | Inhibition of human recombinant AChE preincubated for 20 mins before substrate addition by Ellman's method | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238. |
| AID1702428 | Pseudo-irreversible inhibition of human erythrocytes AChE assessed as enzyme recovery activity at 0.1 times IC50 measured at 60 mins using diluted compound relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1738335 | Displacement of [3H]paroxetine from human SERT expressed in human HEK293 cells incubated for 30 mins by liquid scintillation counting analysis | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer's disease. |
| AID1633179 | Cognitive enhancing effect in Wistar rat model of amyloid beta (1 to 42) oligomer-induced memory impairment model assessed as escape latency time at 5 mg/kg, po for 9 days by Morris water maze test (Rvb = 49.3 to 74 secs) | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1416359 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1694872 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 6 mins followed by substrate addition and measured for 180 secs by Ellman's method | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1191940 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman method | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Design, synthesis and evaluation of chromone-2-carboxamido-alkylbenzylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID48158 | Change in heart rate was detected in anaesthetised cats on administration of the compound | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. |
| AID1308834 | Inhibition of human erythrocytes AchE using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman method | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1261739 | Cognitive enhancing effect in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as swimming speed at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by Morris water maze assay (Rvb = 21 +/- 3.1 | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1379011 | Inhibition of equine serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 180 secs by spectrophotometric analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1217704 | Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1421278 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID635878 | Inhibition of rat liver mitochondrial MAO-B using [14C]-phenylethylamine after 30 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | 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 di |
| AID594990 | Inhibition of human BChE after 20 mins using butyrylthiocholine iodide as a substrate by Ellman's assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | 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. |
| AID1330764 | Inhibition of human AChE mediated aggregation of amyloid beta (1 to 40 residues) at 100 uM incubated for 46-48 hrs by thioflavin-T binding assay relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1707768 | Antiinflammatory activity in LPS-induced human THP-1 cells assessed as reduction in TNFalpha release at 10 uM peincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by EIA | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1846122 | In vivo inhibition of AChE in OF1 mouse brain at 10 micromol/kg, ip and measured after 15 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | A review on ferulic acid and analogs based scaffolds for the management of Alzheimer's disease. |
| AID1736948 | Inhibition of self-induced amyloid beta (1 to 42 residues) (unknown origin) aggregation by thioflavin T based fluorescence assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID763849 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins prior to substrate addition by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1702434 | Inhibition of human erythrocyte AChE-induced amyloid beta 1 to 40 (unknown origin) aggregation at 100 uM by thioflavin-T fluorescence method relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1076766 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 1 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay relat | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1421287 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 50 uM after 24 hrs by MTS assay relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID1736947 | Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity measured every min for 4 hrs by ORAC-FL assay relative to trolox | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1347794 | Inhibition of amyloid beta (25 to 35 residues) (unknown origin)-induced toxicity in rat PC12 cells assessed as protection against amyloid beta (25 to 35 residues)-induced apoptosis by measuring early apoptotic cells at 50 ug/ml by Annexin V-FITC/propidium | |||
| AID1752608 | Displacement of propidium iodide from the PAS site of human AChE at 20 uM preincubated with enzyme for 6 hrs followed by incubation with propidium iodide and measured after 20 mins by fluorescence analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease. |
| AID1374195 | Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells at 10 uM using kynuramine as substrate after 30 mins by fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5 | Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment. |
| AID1555998 | Neuroprotective activity against H2O2 induced cytotoxicity in rat PC12 cells assessed as cell viability at 30 uM pretreated for 3 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay (Rvb = 35.69 to 50.26%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1691667 | Inhibition of human serum BuChE assessed as residual activity at IC50 using acetylcholine iodide as substrate measured after dilution by Ellman's method relative to control | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1533606 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate after 10 mins measured for every mins by Ellman's method | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1738138 | Ex vivo antioxidant activity in brain of scopolamine-induced Swiss albino mouse model of amnesia assessed as increase in CAT level at 5 mg/kg, po administered for 7 days and observed after 30 mins before scopolamine treatment and measured after 15 mins | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID1656474 | In-vivo inhibition of AChE in rat cerebral cortex at 0.1 mg/kg, ip relative to control | 2020 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3 | Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy. |
| AID748749 | Antiamnesic activity in Charles Foster albino rat assessed as reduction in scopolamine-induced increase in transfer latency at 5 mg/kg, po administered for 7 days measured 30 mins post last dose by elevated plus maze task (Rvb = 67.67 +/- 0.88 s) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Design, synthesis and evaluation of some new 4-aminopyridine derivatives in learning and memory. |
| AID1901713 | Inhibition of C-terminal 6His-tagged human recombinant BuChE (29 to 602 residues) using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents. |
| AID1261786 | Cognitive enhancing effect in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as reduction in escape latency at 2 mg/kg/day administered as intragastric infusion for 32 days measured during compound dosing by Morris water maze assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1650983 | Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents. |
| AID1737047 | Antialzheimer activity in scopolamine-induced Kunming mouse model of memory impairment assessed as latency time at 5 mg/kg po by step-down passive avoidance test (Rvb = 125.65 sec) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID30243 | In vitro inhibitory activity against acetylcholinesterase | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | QSAR analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase. |
| AID1556048 | Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in production of H202 using p-tyramine as substrate incubated for 30 mins followed by substrate addition by horse radish peroxidase | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Dipropargyl substituted diphenylpyrimidines as dual inhibitors of monoamine oxidase and acetylcholinesterase. |
| AID1632236 | Antioxidant activity against scopolamine-induced oxidative stress in Albino LACA mouse brain homogenate assessed as lipid peroxidation by measuring malondialdehyde level per mg protein at 1 mg/kg, ip by TBARS assay (Rvb = 1.62 +/- 0.1 mol) | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19 | Coumarin derivatives as potential inhibitors of acetylcholinesterase: Synthesis, molecular docking and biological studies. |
| AID1633174 | Inhibition of human erythrocyte AChE-induced amyloid beta 1 to 42 (unknown origin) aggregation up to 20 uM after 48 hrs by thioflavin T-based fluorometric assay relative to donepezil | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID351914 | Inhibition of human recombinant AChE by Ellman's method | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors. |
| AID1585834 | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1552590 | Permeability of compound at 25 ug/ml at pH 7.4 incubated for 18 hrs by PAMPA-BBB assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID384079 | Inhibition of horse serum butyrylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID1503610 | Selectivity index, ratio of IC50 for human serum AChE to IC50 for human serum BChE | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation. |
| AID384080 | Inhibition of rat brain acetylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID539464 | Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate. |
| AID1732104 | Permeability of the compound measured after 16 hrs by PAMPA-BBB assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | 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. |
| AID1851405 | Inhibition of human serum recombinant BChE using butyrylthiocholine iodide as a substrate incubated for 20 mins by DTNB reagent based Ellman's method | |||
| AID1900710 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID1383666 | Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM after 25 mins | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
| AID1632235 | Antioxidant activity against scopolamine-induced oxidative stress in Albino LACA mouse brain assessed as superoxide dismutase activity by measuring auto oxidation of hydroxylamine hydrochloride per mg protein at 1 mg/kg, ip measured for 2 mins at 30 to 60 | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19 | Coumarin derivatives as potential inhibitors of acetylcholinesterase: Synthesis, molecular docking and biological studies. |
| AID1406161 | Neuroprotective activity against rotenone/oligomycin A-induced mitochondrial oxidative stress in human SH-SY5Y cells at 5 uM after 24 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease. |
| AID1245374 | Inhibition of electric eel AChE using DTNB as substrate incubated for 5 mins prior to substrate addition measured after 2 mins by Ellman's method | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Multifunctional novel Diallyl disulfide (DADS) derivatives with β-amyloid-reducing, cholinergic, antioxidant and metal chelating properties for the treatment of Alzheimer's disease. |
| AID131755 | Tested for effective dose for elevation of Acetylcholinesterase (AChE) in mouse forebrain | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
| AID1764087 | Anti-inflammatory activity in rat PC12 cells assessed as reduction in TCN-induced ER stress by measuring increase in cell viability at 1 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | The structural simplification of lysergic acid as a natural lead for synthesizing novel anti-Alzheimer agents. |
| AID1329700 | Inhibition of acetylcholinesterase (unknown origin) using acetylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition measured after 20 mins by UV-Vis spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1 | Synthesis, structure-activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID1186313 | Inhibition of BChE in rat serum using butyrylthiocholine iodide substrate incubated for 15 mins by UV spectroscopy based Ellman's method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy. |
| AID1353359 | Selectivity ratio of IC50 for BuChE (unknown origin) to IC50 for AChE (unknown origin) | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1784744 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT |
| AID1633182 | Reversal of scopolamine-induced spatial memory impairment in Wistar rat model of amnesia assessed as decrease in time spent on open arms at 5 mg/kg, po administered once daily for 1 week followed by scopolamine challenge 30 mins prior to test by elevated | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1872732 | Inhibition of AChE (unknown origin) incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy. |
| AID670569 | Inhibition of self-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by thioflavin T-based fluorescence analysis | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14 | Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template. |
| AID1506843 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Rational design, synthesis and biological screening of triazine-triazolopyrimidine hybrids as multitarget anti-Alzheimer agents. |
| AID1635495 | Antiapoptotic activity in rat primary hippocampal cells assessed as inhibition of Abeta (1 to 42)-induced apoptosis by measuring early apoptotic cells level at 20 uM incubated for 2 hrs followed by Abeta (1 to 42) challenge measured after 24 hrs by annexi | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID666578 | Selectivity ratio of IC50 for equine serum butyrylcholinesterase to IC50 for electric eel acetylcholine esterase | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents. |
| AID1635514 | Neuroprotective activity in Swiss albino mouse brain assessed as inhibition of scopolamine-induced elevation in BuChE level at 5 mg/kg, po administered 30 mins prior to scopolamine challenge administered for 9 days by Ellman assay relative to vehicle-trea | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1718177 | Inhibition of acetylcholinesterase (unknown origin) | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases. |
| AID594991 | Inhibition of amyloid beta (1-40) aggregation at 100 uM by thioflavin-T based spectrofluorometric assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | 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. |
| AID30679 | Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in bovine erythrocytes | 1998 | Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6 | Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase. |
| AID282831 | Inhibition of beta amyloid protein 40 aggregation at 100 uM by thioflavin T-based fluorometric assay | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease. |
| AID763828 | Cognitive enhancing effect in po dosed Wistar rat assessed as reversal of learning impairment measured as transfer latency administered for 8 days by elevated plus maze test | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1738123 | Memory enhancement effect in scopolamine-induced Swiss albino mouse model of amnesia assessed as increase in spontaneous alteration at 5 mg/kg, po administered for 7 days and observed after 30 mins before scopolamine treatment and measured after 15 mins b | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1360335 | Inhibition of human BchE (unknown origin)-induced amyloid beta (1 to 42) aggregation at 10 uM after 48 hrs by thioflavin T fluorescence method relative to control | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and β-secretase inhibition activities. |
| AID1571069 | Inhibition of electric eel AChE-induced amyloid beta (1 to 42) aggregation at 50 uM after 48 hrs by thioflavin T-based fluorometric assay relative to control | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11 | New amyloid beta-disaggregating agents: synthesis, pharmacological evaluation, crystal structure and molecular docking of |
| AID1736941 | Inhibition of AChE in human erythrocytes by Ellman's method | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1176152 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins at 1 uM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID395657 | Inhibition of AChE in rat cortex after 15 mins by modified Ellman method | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives. |
| AID1851404 | Inhibition of human serum recombinant AChE using acetylthiocholine iodide as a substrate incubated for 20 mins by DTNB reagent based Ellman's method | |||
| AID395660 | Cognitive enhancing effect against scopolamine-induced acquisition memory deficit in mouse assessed as times of step-down at 2 mg/kg, intragastric gavage after 24 hrs by step-down passive avoidance test | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives. |
| AID595289 | Inhibition of human AChE using acetylthiocholine iodide as substrate by Ellman's assay | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1330751 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1702489 | Antialzheimer activity against 3 dpf zebrafish model of AlCl3-induced AD assessed as change in motility distance at 8 uM (Rvb = 5204 mm) | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1612695 | Effect on total entries in ICR mouse model of scopolamine-induced memory impairment at 10 mg/kg by Y-maze test | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone. |
| AID768524 | Inhibition of human plasma BuChE using butyrylthiocholine as substrate by Ellman's method | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis, pharmacological assessment, and molecular modeling of 6-chloro-pyridonepezils: new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease. |
| AID1627645 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellmans method | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands. |
| AID1545272 | Inhibition of human Cholinesterase | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID44288 | Inhibition of butyrylcholinesterase from human serum | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1736946 | Selectivity index, ratio of IC50 for inhibition of human serum BChE to IC50 for inhibition of AChE in human erythrocytes | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1400272 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
| AID482855 | Inhibition of AChE in human erythrocytes by Ellman's method | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
| AID1353379 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability after 6 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1625111 | Inhibition of Cu2+-induced human amyloid beta (1 to 42) aggregation at 25 uM after 24 hrs by thioflavin T-based fluorometric assay relative to control | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities. |
| AID1517852 | Inhibition of HFIP-pretreated amyloid beta (1 to 42 residues) (unknown origin) self aggregation at 25 uM after 24 hrs by ThT-based fluorescence method relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID238665 | Dissociation constant for inhibition of fetal bovine serum Acetylcholinesterase | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. |
| AID1601892 | Inhibition of human erythrocyte AChE using acetylthiocholine as substrate by Ellman's assay | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID1397454 | Inhibition of horse serum BuChE using acetylthiocholine as substrate after 60 mins by FRET assay | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors. |
| AID1702437 | Disaggregation of Copper-induced amyloid beta (1 to 42) (unknown origin) preformed fibrils at 25 uM by ThT fluorescence assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID763838 | Activity at AChE in Charles Foster rat prefrontal cortex assessed as substrate hydrolyzed per mg of protein at 5 mg/kg, po for 8 days by Ellman's method (Rvb = 45.83 +/- 0.94 mol/min) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1533631 | In vivo antioxidant activity in Swiss albino mouse brain assessed as decrease in nitric oxide level at 1 mg/kg, ip qd pretreated for 1 hr followed by scopolamine addition by Griess reagent based assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID351915 | Inhibition of human serum BChE by Ellman's method | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors. |
| AID1359861 | Inhibition of recombinant human AChE-induced amyloid beta (1 to 42) aggregation at 100 uM incubated for 48 hrs by thioflavin-T fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds. |
| AID600980 | Inhibition of human erythrocytes BChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID1784745 | Irreversible inhibition of recombinant equine serum BChE using butyrylthiocholine as substrate preincubated up to 120 mins by DTNB-reagent based 100-fold dilution assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT |
| AID1737042 | Antialzheimer activity in Alcl3-induced zebra fish AD model assessed as increase dyskinesia recovery rate at 8 uM relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1465296 | Inhibition of electric eel AChE using acetylthiocholine as substrate incubated for 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1257002 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 15 mins by Ellman's method | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease. |
| AID1368602 | Inhibition of AchE in brain homogenates of scopolamine-induced albino mouse memory deficit model at 5 uM using acetylthiocholine iodide as substrate incubated for 10 mins measured for 2 mins by Ellman's method relative to control | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1906375 | Neuroprotective activity in human SH-SY5Y differentiated neuronal cells assessed as inhibition of GA-induced axon morphology defects at 5 uM by laser confocal microscope | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1209457 | Unbound Cmax in human plasma | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID364670 | Inhibition of Electrophorus electricus brain AChE by Ellman's method | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues. |
| AID1480846 | Inhibition of human erythrocyte AChE at 5 uM using acetylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID763829 | Cognitive enhancing effect in Wistar rat assessed as reversal of learning impairment measured as transfer latency at 10 mg/kg, po for 8 days measured on second day of test by elevated plus maze test (Rvb = 66.824 +/- 0.47 seconds) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1368605 | Inhibition of AchE in brain homogenates of scopolamine-induced albino mouse memory deficit model at 50 uM using acetylthiocholine iodide as substrate incubated for 10 mins measured for 2 mins by Ellman's method relative to control | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1537658 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate by Ellman's method | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1877965 | Inhibition of human AChE by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease. |
| AID1517851 | Inhibition of Cu2+-induced amyloid beta (1 to 42 residues) aggregation at 25 uM after 24 hrs by thioflavin T-based fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1569985 | Reversible inhibition of equine serum BuChE assessed as enzyme activity at 1xIC50 using butyrylthiocholine iodide as substrate measured after dilution by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1199519 | Inhibition of equine serum BuChE after 5 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID30660 | Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in Torpedo californica | 1998 | Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6 | Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase. |
| AID1152915 | Inhibition of MAO-B in rat liver homogenate using [14C]-phenylethylamine as substrate preincubated for 30 mins followed by substrate addition measured after 4 mins by liquid scintillation counting analysis | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1478776 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for Electric eel AChE | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. |
| AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID496881 | Inhibition of AChE | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy. |
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1126182 | Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins before substrate addition after 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis, cytotoxicity and molecular modelling studies of new phenylcinnamide derivatives as potent inhibitors of cholinesterases. |
| AID1390034 | Inhibition of self-induced aggregation of amyloid beta (1 to 42) (unknown origin) at 25 uM after 24 hrs by thioflavin T fluorescence-based fluorometric method relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
| AID759421 | Inhibition of human BuChE using S-butyrylthiocholine iodide as substrate treated 5 mins before substrate addition measured up to 4 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Selective inhibition of human acetylcholinesterase by xanthine derivatives: in vitro inhibition and molecular modeling investigations. |
| AID1736860 | Inhibition of human plasma BuChE using butyrylthiocholine as substrate measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | 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. |
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1900709 | Inhibition of equine serum BChE at 50 uM using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1311918 | Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity preincubated for 15 mins followed by AAPH addition measured every min for 120 mins by ORAC-FL assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1766052 | Inhibition of human GluN1-1a/NR2B receptor expressed in transgenic mouse fibroblast cells assessed as inhibition of L-glutamate-induced excitotoxicity at 20 uM by measuring LDH activity by cell based assay | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors. |
| AID1767558 | Selectivity index, ratio of IC50 for human BuChE to IC50 for human AChE | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant. |
| AID1421285 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 10 uM after 24 hrs by MTS assay relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID1772656 | Ex vivo inhibition of AChE in ICR mouse brain at 5 uM measured after 1 hr by Ellman method relative to control | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID1421288 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 10 uM after 48 hrs by MTS assay relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID1466565 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | |||
| AID1702423 | Pseudo-irreversible inhibition of human erythrocytes AChE assessed as enzyme recovery activity at 0.1 times IC50 using diluted compound relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1757183 | Inhibition of rat cortex homogenate acetylcholinesterase by Ellman's method | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease. |
| AID1530605 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Investigating alkyl nitrates as nitric oxide releasing precursors of multitarget acetylcholinesterase-monoamine oxidase B inhibitors. |
| AID1702418 | Selectivity index, ratio of IC50 for rat serum butyrylcholinesterase to IC50 for rat cortex acetylcholinesterase | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1252806 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | New multifunctional melatonin-derived benzylpyridinium bromides with potent cholinergic, antioxidant, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1311917 | Inhibition of self-induced aggregation of amyloid beta (1 to 42) (unknown origin) at 20 uM measured after 46 to 48 hrs by ThT-based fluorometric assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID462788 | Inhibition of human recombinant AChE-induced amyloid beta (1-40) aggregation at 100 uM after 48 hrs by thioflavin T fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238. |
| AID1400271 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
| AID1698419 | Displacement of propidium iodide from PAS region of human AChE at 50 uM incubated for 6 hrs by fluorescence assay relative to control | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1167544 | Mixed-type inhibition of human erythrocyte AChE by Lineweaver-Burk reciprocal plot method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1267382 | Selectivity ratio of IC50 for horse serum BuChE to IC50 for electric eel AChE | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents. |
| AID1352676 | Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1691727 | Antialzheimer activity in AlCl3-induced Zebrafish model of Alzheimer's disease assessed as increase in motility distance at 8 uM relative to control | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1633232 | Inhibition of mouse plasma BuChE using S-butyrylacetylthiocholine iodide as substrate measured after 30 mins by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1217729 | Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1674988 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by UV-vis spectrophotometry based Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Discovery of biphenyl pyrazole scaffold for neurodegenerative diseases: A novel class of acetylcholinesterase-centered multitargeted ligands. |
| AID1635485 | Selectivity ratio of IC50 for human erythrocyte AChE to IC50 for equine serum BuChE | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1767555 | Inhibition of human AchE-induced amyloid beta (25 to 35)aggregation at 100 uM after 48 hrs by ThT fluorescence assay relative to control | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant. |
| AID1569980 | Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1311920 | Inhibition of human serum BCHE preincubated for 6 mins followed by addition of S-butyrylcholine iodide as substrate by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1709253 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1261752 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as irregular shape in dentate gyrus region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hem | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1633197 | Antioxidant activity Wistar rat model of scopolamine-induced amnesia assessed as increase in in SOD levels in brain homogenates at 5 mg/kg, po by NBT dye based assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1292352 | Inhibition of amyloid beta (1-42) (unknown origin) self-induced aggregation at 10 uM after 2 days by thioflavin T fluorometric assay relative to control | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Biological evaluation of synthetic α,β-unsaturated carbonyl based cyclohexanone derivatives as neuroprotective novel inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID1609210 | Neuroprotective activity against amyloid beta (1 to 42)-induced cytotoxicity in human SH-SY5Y cells assessed as increase in cell viability at 10 to 20 uM measured after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1176167 | Oral bioavailability in human | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1764084 | Neuroprotective activity against rat PC12 cells under glucose and oxygen-deprived condition assessed as increase in cell viability at 0.1 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | The structural simplification of lysergic acid as a natural lead for synthesizing novel anti-Alzheimer agents. |
| AID1338168 | Inhibition of BuChE (unknown origin) at 1 uM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease. |
| AID1444069 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1569990 | Disaggregation of Cu2+ induced preformed fibrils of amyloid beta (1 to 42) (unknown origin) at 25 uM after 24 hrs by transmission electron microscopy relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1635489 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 80 uM after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1882053 | Inhibition of recombinant bovine mitochondrial MAO-B using benzylamine or serotonin as substrate incubated for 60 mins by fluorimetry assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
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| AID1884592 | Anti-neuroinflammatory activity against LPS-stimulated mouse BV-2 cells assessed as reduction in TNF-alpha production at 20 uM pretreated for 1 hr with compound followed by LPS treatment for 24 hrs by ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID1404011 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors. |
| AID1220559 | Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
| AID1070083 | Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease. |
| AID1501669 | Cytoprotection against amyloid beta (1 to 42) peptide induced cell death in human SH-SY5Y cells assessed as increase in clonogenic survival at 0.0057 uM after 24 hrs by Giemsa staining-based inverted microscopic analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID1557170 | Inhibition of equine serum BuChE using S-butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19 | The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID657796 | Inhibition of mitochondrial MAO-A in rat liver homogenates using [14C]-(5-hydroxy-triptamine) as substrate preincubated for 30 mins by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 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. |
| AID1352673 | Antialzheimer activity in scopolamine induced cognitive deficit Kunming mouse model assessed as latency time at 5 mg/kg, po treated for 1 hr followed by training trial and subsequent addition of scopolamine at 30 mins post trial measured for 24 hrs interv | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1700051 | Inhibition of human serum BuChe by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation. |
| AID1055213 | Inhibition of human recombinant AChE-induced amyloid beta (1 to 40) aggregation at 100 uM after 48 hrs by thioflavin T fluorescence assay relative to control | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID1176161 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 10 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1517855 | Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID594820 | Inhibition of AChE-induced amyloid beta aggregation | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | (+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase. |
| AID1484814 | Inhibition of rat cortex homogenate AChE using acetylthiocholine iodide as substrate after 15 mins in presence of BuChE inhibitor iso-OMPA by Ellman's method | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1191628 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate incubated for 5 mins by Ellman's method | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Synthesis, biological evaluation and molecular docking study of novel piperidine and piperazine derivatives as multi-targeted agents to treat Alzheimer's disease. |
| AID1576119 | Neuroprotective activity against amyloid beta (1 to 42)-induced neurotoxicity in Sprague-Dawley rat hippocampal neuron assessed as cell survival rate at 1 uM incubated for 48 hrs in presence of amyloid beta (1 to 42) by CellTiter Glo-based luminescence as | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | The synthesis and biological evaluation of novel gardenamide A derivatives as multifunctional neuroprotective agents. |
| AID1209456 | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID1166296 | Inhibition of electric eel AChE by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Active compounds from a diverse library of triazolothiadiazole and triazolothiadiazine scaffolds: synthesis, crystal structure determination, cytotoxicity, cholinesterase inhibitory activity, and binding mode analysis. |
| AID1338124 | Permeability of the compound at 100 uM up to 6 hrs by PAMPA | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation. |
| AID1466564 | Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis | |||
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| AID1568793 | Reversible inhibition of equine serum BuChE assessed as enzyme activity at IC50 using butyrylthiocholine iodide as substrate by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
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| AID1702419 | Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1623119 | Drug metabolism in Sprague-Dawley rat liver microsomes assessed as metabolic rate up to 180 mins in presence of NADPH by UV-based LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1596161 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Jul-15, Volume: 174 | Benzoic acid-derived nitrones: A new class of potential acetylcholinesterase inhibitors and neuroprotective agents. |
| AID482856 | Inhibition of electric eel AChE by Ellman's method | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
| AID1453099 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease. |
| AID1498850 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 2 mins followed by substrate addition and measured after 2 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Design, synthesis and evaluation of novel bivalent β-carboline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1809148 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, synthesis, and cholinesterase inhibition assay of liquiritigenin derivatives as anti-Alzheimer's activity. |
| AID1693557 | Inhibition of recombinant human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 cells using prephosphorylated polypeptide as substrate incubated for 1 min followed by substrate addition and measured after 30 mins by Kin | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID1191627 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Synthesis, biological evaluation and molecular docking study of novel piperidine and piperazine derivatives as multi-targeted agents to treat Alzheimer's disease. |
| AID1707764 | Reversible inhibition of recombinant human BChE assessed as residual activity at IC50 using butyrylthiocholine iodide as substrate preincubated for 30 mins followed by 100-fold dilution in presence of substrate and measured after 15 mins by Ellman's metho | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1501666 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID1736938 | Inhibition of equine serum BChE by Ellman's method | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1633201 | Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1879287 | Inhibition of electric eel AChE | 2022 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 61 | 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. |
| AID1678836 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by Ellman's method | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease. |
| AID1125768 | Selectivity ratio of IC50 for BuChE in equine serum to IC50 for electric eel AChE | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Quinolone-benzylpiperidine derivatives as novel acetylcholinesterase inhibitor and antioxidant hybrids for Alzheimer disease. |
| AID1152940 | Cognitive enhancing effect in C57BL/6J mouse assessed as reversal of scopolamine-induced long-term memory deficit by measuring increase in latency time during probe session at 1 mg/kg, iv administered 90 mins prior to scopolamine-challenge measured after | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1176165 | Fraction unbound in Sprague-Dawley rat at 5 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1167540 | Inhibition of electric eel AChE preincubated for 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1325671 | Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Design, synthesis, and AChE inhibitory activity of new benzothiazole-piperazines. |
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| AID1517837 | Reversal of scopolamine-induced memory impairment in Kunming mouse assessed as increase in latency time at 5 mg/kg, po treated with compound 1 hr before training trial followed by 30 mins later administration with scopolamine and measured 24 hrs after tra | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
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| AID1360334 | Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 10 uM after 48 hrs by thioflavin-T fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and β-secretase inhibition activities. |
| AID1480848 | Inhibition of human serum BuChE at 5 uM using butylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID677023 | Antiamnesic activity in mouse assessed as inhibition of scopolamine-induced escape latency time at 25 mg/kg, ip measured on day 4 by Morris water maze test (Rvb = 78.7 +/- 5.7 secs) | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis and evaluation of novel 4-[(3H,3aH,6aH)-3-phenyl)-4,6-dioxo-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazol-5(3H,6H,6aH)-yl]benzoic acid derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents. |
| AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
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| AID1709522 | Anti-VaD activity against BCCAO-induced Sprague-Dawley rat model of spatial memory deficit assessed as improvement in spatial learning and memory by measuring increase in time spent in target quadrant at 1 mg/kg, ig administered for 2 weeks followed by su | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Twin drug design, synthesis and evaluation of diosgenin derivatives as multitargeted agents for the treatment of vascular dementia. |
| AID31021 | Evaluated for the in vitro inhibition of the Acetylcholinesterase (AChE) from human erythrocytes | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
| AID1633191 | Cognitive enhancing effect in Wistar rat model of amyloid beta (1 to 42) oligomer-induced memory impairment model assessed as increase in number of platform crossings at 5 mg/kg, po for 9 days by Morris water maze test | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1308836 | Mixed inhibition of human erythrocytes AchE using acetylthiocholine iodide as substrate incubated for 20 mins by Lineweaver-Burk plot analysis | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1772658 | Ex vivo inhibition of AChE in ICR mouse brain at 40 uM measured after 1 hr by Ellman method relative to control | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
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| AID1339449 | Cognition enhancement activity in Charles Foster albino rat model of spatial reference memory assessed as decrease in escape latency at 10 mg/kg, po administered from day 1 to 2 measured 1 hr post last dose on day 2 by Morris water maze test | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1772664 | Improvement in learning and spatial memory in amyloid beta (1 to 42)-induced mouse model of Alzheimer's disease assessed as increase in spontaneous alteration at 10 mg/kg/day, po pretreated with amyloid beta42 for 3 days followed by treatment with compoun | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
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| AID1698429 | Cognitive enhancing effect in scopolamine-induced Wistar rat model of amnesia assessed as effect on total arm entries at 5 mg/kg, po pretreated for 7 days followed by scopolamine challenge by Y-maze test | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1400287 | Reversal of scopolamine-induced memory impairment in albino Wistar rat assessed as effect on swimming speed at 2.5 mg/kg, ip by Morris water maze test | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
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| AID1152944 | Apparent permeability in MDCK cells | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1682155 | In vivo inhibition of acetylcholinesterase in rat at 0.038 micromol/kg, icv relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1484832 | Metal chelating activity assessed as disaggregation of Cu2+ induced amyloid beta (1 to 42) fibrils at 25 uM treated for 24 hrs post Cu2+ treatment for 24 hrs by ThT-based fluorometric method relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
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| AID1901724 | Ex vivo inhibition of AChE in Sprague-Dawley rat brain homogenate assessed as residual activity at 10 mg/kg, ip measured after 1 hr by ELISA | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents. |
| AID1702436 | Disaggregation of self-induced amyloid beta (1 to 42) (unknown origin) preformed fibrils at 25 uM by ThT fluorescence assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID511766 | Inhibition of human AChE by Ellmans test | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based virtual screening, synthesis, and pharmacology. |
| AID1484815 | Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1404012 | Inhibition of recombinant human serum BuChE using butyrylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors. |
| AID1368604 | Inhibition of AchE in brain homogenates of scopolamine-induced albino mouse memory deficit model at 25 uM using acetylthiocholine iodide as substrate incubated for 10 mins measured for 2 mins by Ellman's method relative to control | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1390041 | Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
| AID1501662 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 0.0057 uM after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID595291 | Selectivity ratio of IC50 for human BChE to IC50 for human AChE | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
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| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
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| AID1865084 | Inhibition of human recombinant AChe using acetylthiocholine iodide as substrate incubated for 10 mins by DTNB reagent based Ellman's method | |||
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| AID1427877 | Oral bioavailability in human | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Targeting Alzheimer's disease by investigating previously unexplored chemical space surrounding the cholinesterase inhibitor donepezil. |
| AID1756685 | Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as off rate constant at 298.15 K by surface plasmon resonance assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
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| AID1353363 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1444074 | Inhibition of AChE in rat cortex homogenates using acetylthiocholine chloride as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1597699 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | 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. |
| AID1673634 | Inhibition of human BACE-1 using MOCA-SEV-NL-DAEFR-DNP-RR as substrate preincubated with substrate followed by enzyme addition by FRET assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1767557 | Inhibition of recombinant human BuChe using S-butyrylthiocholine iodide as substrate measured after 7 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant. |
| AID1191631 | Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity at 1 to 10 uM preincubated for 15 mins followed by AAPH challenge measured every min for 80 mins by ORAC-FL assay | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Synthesis, biological evaluation and molecular docking study of novel piperidine and piperazine derivatives as multi-targeted agents to treat Alzheimer's disease. |
| AID1596165 | Noncompetitive inhibition of electric eel AChE assessed as decrease in Vmax of substrate at 12.5 nM to 50 nM using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured for 5 mins by double reciprocal Lineweave | 2019 | European journal of medicinal chemistry, Jul-15, Volume: 174 | Benzoic acid-derived nitrones: A new class of potential acetylcholinesterase inhibitors and neuroprotective agents. |
| AID1824585 | Inhibition of hERG expressed in CHO cells at -80 mV holding potential by automated patch clamp method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1416382 | Reversal of scopolamine-induced memory impairment in Kunming mouse assessed as step down latency time at 5 mg/kg, po treated for 1 hr before training followed by scopolamine challenge 30 mins before training measured 24 hrs after training trial by passive | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1152932 | Hepatotoxicity in human HepG2 cells assessed as cell viability at 1 uM by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1784498 | Inhibition of amyloid beta (1 to 42) (unknown origin) aggregation in Escherichia coli BL21 (DE3) at 10 uM incubated overnight by thioflavin S based fluorescence analysis relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | 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. |
| AID1245375 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Multifunctional novel Diallyl disulfide (DADS) derivatives with β-amyloid-reducing, cholinergic, antioxidant and metal chelating properties for the treatment of Alzheimer's disease. |
| AID1055868 | Inhibition of electric eel AChE using acetylcholine as substrate preincubated for 15 mins prior to substrate addition by Ellman's method | 2013 | European journal of medicinal chemistry, , Volume: 70 | Novel coumarin-3-carboxamides bearing N-benzylpiperidine moiety as potent acetylcholinesterase inhibitors. |
| AID1406140 | Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease. |
| AID262754 | Anticholinesterase activity against human erythrocyte AChE | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
| AID1578224 | Antagonist activity at histamine H3 receptor (unknown origin) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Search for new multi-target compounds against Alzheimer's disease among histamine H |
| AID1322994 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate measured for 2 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and anticholinesterase activity of coumarin-3-carboxamides bearing tryptamine moiety. |
| AID1635492 | Antioxidant activity assessed as DPPH free radical scavenging activity at 10 uM after 30 secs by spectrophotometry | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1633172 | Displacement of Propidium iodide from PAS region of AChE (unknown origin) at 50 uM incubated for 6 hrs by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1459562 | Inhibition of equine serum BuChE using S-butylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1201373 | Selectivity index, ratio of IC50 for equine serum butyrylcholine esterase to IC50 for electric eel AChE | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Blood-brain barrier permeable anticholinesterase aurones: synthesis, structure-activity relationship, and drug-like properties. |
| AID1359855 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition by Ellman's method | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds. |
| AID1338142 | Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity at 1 to 25 uM preincubated for 15 mins followed by AAPH addition measured every min for 80 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis, in-silico and biological evaluation of novel donepezil derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1767556 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate measured after 7 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant. |
| AID1191939 | Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman method | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Design, synthesis and evaluation of chromone-2-carboxamido-alkylbenzylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1126627 | Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins before substrate addition after 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | 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. |
| AID1503606 | Inhibition of human serum AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation. |
| AID1352654 | Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM measured after 46 to 48 hrs by ThT fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1407192 | Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production at 10 to 30 uM after 24 hrs by Griess assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID1407208 | Reversal of scopolamine-induced memory impairment in ICR mouse assessed as increase in step-through latency time at 5 mg/kg, po administered for 10 consecutive days and 60 mins prior to training trial followed by scopolamine challenge at 30 mins post dose | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID1176164 | Total steady state plasma concentration in Sprague-Dawley rat at 5 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1771842 | Inhibition of BuChE in human plasma using BTC as substrate at 10 uM preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT |
| AID1691726 | Antialzheimer activity in AlCl3-induced Zebrafish model of Alzheimer's disease assessed as motility distance at 8 uM (Rvb = 5346 mm) | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1866878 | Selectivity index, ratio of IC50 for equine serum BchE to IC50 for Electrophorus electricus AchE | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors. |
| AID1657148 | Inhibition of BuChE in rat serum using S-butylthiocholine iodide as substrate by Ellman's method | 2020 | Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8 | Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. |
| AID763839 | Cognitive enhancing effect in Charles Foster rat assessed as reversal of scopolamine-induced amnesia measured as transfer latency at 10 mg/kg, po for 8 days administered 1 hr prior to scopolamine-challenge on day 7 measured on day 8 by elevated plus maze | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1501303 | Antiproliferative activity against human SK-N-MC cells at 10 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1682161 | In vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex at 8 micromol/kg, IG administered once daily for 8 days and measured 30 mins post 8th dose by spectrophotometric method relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1739255 | Selectivity index, ratio of IC50 for BuChE (unknown origin) to IC50 for AChE (unknown origin) | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase. |
| AID1465278 | Inhibition of rat serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | 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. |
| AID227060 | IC50 (hBuChE/hAChE) ratio of the compound | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. |
| AID1077084 | Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1609494 | Cognitive enhancing effect in Swiss albino mouse model of STZ-induced cognition deficit assessed as reduction in escape latency time to find removed platform position at 5 mg/kg, po administrated for 15 days and measured for 4 days by Morris water maze te | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives. |
| AID1736968 | Inhibition of human AChE assessed as residual activity at IC50 concentration relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1736863 | Selectivity ratio of IC50 for human erythrocyte AChE to IC50 for human plasma BuChE | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | 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. |
| AID1453101 | Inhibition of 5% rat cortex homogenate AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID635811 | Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation at 1 uM after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID1820952 | Reversible inhibition of equine serum BChE assessed as residual enzyme activity using butyrylthiocholine iodide as substrate at 1 times IC50 incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1279142 | Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1756760 | Cognitive enhancing effect in mouse model of scopolamine-induced memory impairment assessed as reduction in number of errors at 8 to 12 mg/kg, IG QD for 3 days by channel water maze test | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1444085 | Disaggregation of amyloid beta (1 to 42) (unknown origin) self aggregation at 25 uM after 24 hrs by thioflavin-T assay relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID725909 | Inhibition of AChE in Sprague-Dawley rat cortices using acetylthiocholine iodide as substrate by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors. |
| AID1152937 | Hepatotoxicity in human HepG2 cells assessed as cell viability at 300 uM by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1809145 | Selectivity index, ratio of IC50 for equine serum BuChE using butyrylthiocholine chloride as substrate to IC50 for electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 to 20 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, synthesis, and cholinesterase inhibition assay of liquiritigenin derivatives as anti-Alzheimer's activity. |
| AID1738109 | Displacement of propidium iodide from human AChE at 20 uM incubated for 6 hrs followed by propidium iodide addition and measured after 20 mins by fluorescence based assay relative to control | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID677013 | Inhibition of AChE activity in rat brain homogenate using acetylthiocholine as substrate by Ellman's method | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis and evaluation of novel 4-[(3H,3aH,6aH)-3-phenyl)-4,6-dioxo-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazol-5(3H,6H,6aH)-yl]benzoic acid derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents. |
| AID1581346 | Neuroprotective activity in mouse model of LPS-induced induced memory impairment assessed as improvement in discrimination index at 1 mg/kg, ip by novel object recognition test | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
| AID1587301 | Memory improvement effect in trained unilateral common carotid artery occlusion-induced C57BL/6J mouse model of vascular dementia assessed as increase in removed platform area crossings at 0.7 mg/kg, ig after 21 days by Morris water maze test | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia. |
| AID1673643 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation assessed as normalized fluorescence intensity at 5 to 20 uM after 48 hrs by Thioflavin T based fluorometric assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1865086 | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by scintillation counting method | |||
| AID1707765 | Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity at 10 uM measured every min for 90 mins by ORAC-FL assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1068377 | Inhibition of human AChE using acetylthiocholine as substrate by Ellman's method | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease. |
| AID1290891 | Inhibition of human erythrocyte acetylcholinesterase-mediated amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by thioflavin T fluorescence method | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease. |
| AID1383642 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured for 20 mins at 1 min interval by Ellman's method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
| AID1478778 | Inhibition of human AChE mediated aggregation of amyloid beta (1 to 42 residues) measured after 24 hrs by thioflavin-T fluorescence assay (Rvb = 128.5%) | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. |
| AID1261763 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as condensed cytoplasm in dentate gyrus region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1308835 | Inhibition of horse serum BuChE using butyrylthiocoline iodide as substrate incubated for 20 mins by Ellman method | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1261772 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as reduction of dead neurons in CA3 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hem | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1465284 | Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | 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. |
| AID1480842 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-aggregation at 20 uM after 48 hrs by thioflavin T fluorescence assay relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID482894 | Inhibition of AChE | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Prediction of acetylcholinesterase inhibitors and characterization of correlative molecular descriptors by machine learning methods. |
| AID1702426 | Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at 0.1 times IC50 using diluted compound relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1317854 | Selectivity ratio, ratio of IC50 for equine serum BuChE to electric eel AChE | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID1290888 | Selectivity index, ratio of IC50 for rat serum butyrylcholinesterase to IC50 for Electrophorus electricus acetylcholinesterase | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease. |
| AID1416366 | Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 to 3 mins time interval by Ellman's method | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1320870 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | 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. |
| AID1609206 | Displacement of propidium iodide from PAS region of electric eel AChE at 10 uM incubated for 6 hrs by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1532591 | Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min time interval for 10 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
| AID1633204 | Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells at 10 uM incubated for 30 mins by beta-lactamase complementation technology relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID511767 | Antidementia against scopolamine-induced cognitive impairment in Swiss albino mouse assessed as improvement in latency to transfer from bright to dark compartment at 20 umol/kg, po by passive avoidance test | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based virtual screening, synthesis, and pharmacology. |
| AID1691664 | Inhibition of human serum BuChE assessed as residual activity at 0.1 times IC50 using acetylcholine iodide as substrate measured 120 mins post dilution by Ellman's method relative to control | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1330754 | Inhibition of human serum BuChE using s-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1820989 | Anti-alzheimer activity against scopolamine-induced cognitive dysfunction mouse model assessed as upregulation of AChE activity in hippocampus at 5 mg/kg, po measured after 10 days by colorimetric analysis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1353381 | Cytotoxicity against human HepG2 cells assessed as cell viability at 20 to 40 uM after 6 hrs by trypan blue exclusion assay relative to control | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1623099 | Half life in Sprague-Dawley rat liver microsomes in presence of NADPH by UV-based LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1445548 | Inhibition of propidium iodide binding to electric eel AChE at 1 uM after 6 hrs by fluorescence assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a "Bio-Oxidizable" Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation. |
| AID1506842 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by spectroscopy based Ellman's method | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Rational design, synthesis and biological screening of triazine-triazolopyrimidine hybrids as multitarget anti-Alzheimer agents. |
| AID1693623 | Cognitive enhancing effect in ICR mouse model of scopolamine-induced cognitive dysfunction assessed as reduction in escape latency time to find removed platform position at 15 mg/kg, po by Morris water maze test | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID1167541 | Inhibition of equine BChE preincubated for 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1877995 | Antialzheimer activity against scopolamine-induced cognitive deficit mouse model assessed as increase in AChE content at 5.0 mg/kg, IG by step-through passive avoidance test | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease. |
| AID1568791 | Reversible inhibition of equine serum BuChE assessed as enzyme activity at 0.1 times IC50 using butyrylthiocholine iodide as substrate by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID763845 | Non competitive inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Lineweaver-Burk plot analysis | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1359860 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 100 uM incubated for 48 hrs by thioflavin-T fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds. |
| AID1339439 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1695764 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by DTNB reagent based Ellman's method | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions. |
| AID1605560 | Anti-VaD activity against UCCAO-induced spatial memory deficient C57BL/6J mouse model assessed as improvement in spatial learning and memory by measuring increase in frequency of platform area crossings at 0.7 mg/kg, po administered for 21 days by Morris | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia. |
| AID1757190 | Inhibition of human AchE-induced amyloid beta (1 to 42) (unknown origin) aggregation at 100 uM by ThT fluorescence assay relative to control | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease. |
| AID392812 | Inhibition of human recombinant C-terminal histidine-tagged BACE1 expressed in baculovirus-infected insect cells at 50 ug/mL by FRET assay | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase. |
| AID1826353 | Inhibition of human recombinant AChE by Ellman's spectrophotometric assay | |||
| AID1517860 | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1729623 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate peincubated for 5 mins followed by substrate addition by DTNB-reagent based Ellman's method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT |
| AID1416360 | Inhibition of recombinant human MAO-B assessed as reduction in H2O2 production using p-tyramine as substrate preincubated for 15 mins followed by substrate addition by Amplex red reagent based fluorescence assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1766050 | Inhibition of human GluN1-1a/NR2A receptor expressed in transgenic mouse fibroblast cells assessed as inhibition of L-glutamate-induced excitotoxicity at 50 uM by measuring LDH activity by cell based assay | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors. |
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1762431 | Inhibition of recombinant human BACE1 expressed in baculovirus expression system using Rh-EVNLDAEFK-quencher as substrate incubated for 60 mins by FRET assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters. |
| AID1367031 | Reversal of scopolamine-induced memory impairment in Swiss albino mouse assessed as attenuation of scopolamine-induced amnesia at 2 mg/kg, ip administered 30 mins prior to scopolamine challenge measured on day 4 by Morris water maze test | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Exploration of multi-target potential of chromen-4-one based compounds in Alzheimer's disease: Design, synthesis and biological evaluations. |
| AID1456007 | Antioxidant activity in human SH-SY5Y cells assessed as reduction in H2O2-induced reactive oxygen species formation measured after 24 hrs by DCFH-DA probe based fluorescence assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
| AID1882054 | Selectivity ratio of IC50 for recombinant bovine mitochondrial MAO-B to IC50 for recombinant bovine mitochondrial MAO-A | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID1245372 | Antioxidant activity assessed as trolox equivalents of AAPH radical scavenging activity preincubated for 15 mins followed by AAPH addition measured every min for 80 mins by fluorescein-based ORAC assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Multifunctional novel Diallyl disulfide (DADS) derivatives with β-amyloid-reducing, cholinergic, antioxidant and metal chelating properties for the treatment of Alzheimer's disease. |
| AID1702422 | Pseudo-irreversible inhibition of human erythrocytes AChE assessed as enzyme recovery activity at IC50 using diluted compound relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1578227 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Search for new multi-target compounds against Alzheimer's disease among histamine H |
| AID1736964 | Reversible inhibition of human AChE assessed as residual activity at IC50 concentration relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1472426 | Drug uptake in Wistar Han rat plasma at 10 mg/kg, ip after 1 hr by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1 | The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity. |
| AID1383665 | Inhibition of electric eel AChE-induced amyloid beta (1 to 42) aggregation at 20 uM after 48 hrs by thioflavin T fluorescence spectroscopic method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
| AID1390595 | Cognition enhancing effect in scopolamine-induced cognitive impairment rat model assessed as increase in time spent exploring novel object over familiar object by novel object recognition assay | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6 | Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species. |
| AID1444077 | Inhibition of AChE in human erythrocytes using acetylthiocholine chloride as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1552604 | In vivo antioxidant activity in albino mouse assessed as increase in scopolamine-induced SOD level in brain at 5 mg/kg, po administered once daily for 7 days followed by scopolamine challenge and measured for 2 mins at 30 secs interval | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1626718 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 5 mins by spectrophotometric Ellman's method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Exploring Basic Tail Modifications of Coumarin-Based Dual Acetylcholinesterase-Monoamine Oxidase B Inhibitors: Identification of Water-Soluble, Brain-Permeant Neuroprotective Multitarget Agents. |
| AID1077088 | Inhibition of human erythrocytes AchE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1704848 | Memory enhancement effect in dizocilpine-induced Wistar (Krf:WI) rat model of amnesia assessed as increase in step through latency at 1 mg/kg, ip measured after 30 to 45 mins by step-through passive avoidance test | |||
| AID635879 | Selectivity ratio of IC50 for rat liver mitochondrial MAO-B to IC50 for rat liver mitochondrial MAO-A | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | 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 di |
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| AID1436056 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease. |
| AID1152916 | Selectivity index, ratio of IC50 for MAO-B in rat liver homogenate to IC50 for MAO-A in rat liver homogenate | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID44284 | Concentration required to inhibit 50% of Butyrylcholinesterase obtained from human serum was determined in vitro | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors. |
| AID768525 | Inhibition of purified human erythrocyte AChE using acetylcholine as substrate by Ellman's method | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis, pharmacological assessment, and molecular modeling of 6-chloro-pyridonepezils: new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease. |
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| AID1555986 | Inhibition of self-mediated amyloid beta (1 to 42) (unknown origin) aggregation at 100 uM incubated for 48 hrs by transmission electron microscopic method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1673640 | Permeability of the compound in PBS/EtOH buffer (7:3) at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1555995 | Neuroprotective activity against H2O2 induced cytotoxicity in rat PC12 cells assessed as cell viability at 1 uM pretreated for 3 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay (Rvb = 35.69 to 50.26%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID682340 | Inhibition of human serum BChE using butyrylthiocholine as substrate by Ellman method | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: synthesis, biological assessment, and molecular modeling. |
| AID1176159 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 0.1 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
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| AID1273122 | Inhibition of human carboxylesterase 1 using o-nitrophenylacetate as substrate by spectrophotometry analysis | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors. |
| AID1427875 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Targeting Alzheimer's disease by investigating previously unexplored chemical space surrounding the cholinesterase inhibitor donepezil. |
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| AID1501305 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured for 5 mins by UV spectrophotometric analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1338135 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for Electric eel AChE | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis, in-silico and biological evaluation of novel donepezil derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1732085 | Selectivity index, ratio of IC50 for BuChE in human serum to IC50 for AChE in human erythrocytes measured by DTNB reagent based Ellman's method | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | 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. |
| AID1736867 | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | 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. |
| AID1889347 | Reversible inhibition of human AChE assessed as enzyme recovery activity at undiluted IC50 concentration relative to control | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1605559 | Anti-VaD activity against UCCAO-induced spatial memory deficient C57BL/6J mouse model assessed as improvement in spatial learning and memory by measuring reduction in escape latency at 0.7 mg/kg, po administered for 21 days by Morris water maze test | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia. |
| AID1456003 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured at 12 secs interval for 5 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
| AID1352649 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
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| AID1533625 | In vivo antioxidant activity in Swiss albino mouse brain assessed as decrease in MDA level at 1 mg/kg, ip qd pretreated for 1 hr followed by scopolamine addition by TBARS assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1257004 | Inhibition of self-induced amyloid beta (1-42) aggregation (unknown origin) at 25 uM after 48 hrs by thioflavin T fluorescence method | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease. |
| AID1889700 | Permeability of compound at pH 7.4 by PAMPA assay | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Novel D |
| AID1230944 | Inhibition of human serum BuChE by spectrophotometric Ellman's method | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14 | Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases. |
| AID1736952 | Disaggregation of Cu2+ induced amyloid beta (1 to 42 residues) (unknown origin) aggregation at 25 uM by thioflavin-T fluorescence method relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
| AID1705717 | Inhibition of equine serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every minute for 10 mins by DTNB-reagent based Ellman's method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase. |
| AID1820991 | Anti-alzheimer activity against scopolamine-induced cognitive dysfunction mouse model assessed as change in neuron damage in hippocampal CA3 region at 5 mg/kg, po measured after 10 days by Nissl staining based assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1456008 | Antioxidant activity in human SH-SY5Y cells assessed as reduction in H2O2-induced reactive oxygen species formation at 40 uM measured after 24 hrs by DCFH-DA probe based fluorescence assay relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
| AID1761236 | Permeability of compound at pH 7.4 measured after 6 hrs by PAMPA assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | 2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease. |
| AID1195130 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins by Ellman method | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with β-amyloid anti-aggregation properties and beneficial effects on memory in vivo. |
| AID1517861 | Selectivity index, ratio of IC50 for equine BuChE to IC50 for electric eel AChE | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID44452 | Compound was evaluated for the in vitro inhibition of the Butyrylcholinesterase from horse serum | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
| AID1556047 | Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in production of H202 using p-tyramine as substrate incubated for 30 mins followed by substrate addition by horse radish peroxidase | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Dipropargyl substituted diphenylpyrimidines as dual inhibitors of monoamine oxidase and acetylcholinesterase. |
| AID1752613 | Permeability of the compound in PBS buffer at pH 7.4 at 500 uM incubated for 18 hrs by PAMPA-BBB assay | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease. |
| AID1627646 | Inhibition of equine serum BChE using butyrylthiocholine chloride as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellmans method | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands. |
| AID1900714 | Inhibition of GSK3-beta (unknown origin) incubated for 60 mins by ATP-Glo luminescent assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID1552595 | Cognitive enhancing effect in albino mouse assessed as reversal of scopolamine-induced reduction in spontaneous alteration score at 5 mg/kg, po administered once daily for 7 days followed by scopolamine challenge for 5 mins prior to test and measured on d | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1055216 | Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
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| AID1757185 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease. |
| AID1152908 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 25 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1884594 | Anti-neuroinflammatory activity against aggregated Abeta(25-35)-induced Alzheimer's disease C57BL/6 mouse model assessed as inhibition of TNF-alpha production in hippocampus at 2 mg/kg, iv measured after 2 hrs by ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID1552598 | Reversal of scopolamine-induced amnesic effect in albino mouse assessed as increase in transfer latency time of retention trial at 5 mg/kg, po administered once daily for 7 days followed by scopolamine challenge and subsequent training session for 5 mins | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1195741 | Inhibition of human MAO-B expressed in baculovirus infected BTI insect cells preincubated for 15 mins | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | 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. |
| AID1824584 | Permeability of compound by PAMPA-BBB assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1732083 | Inhibition of AChE in human erythrocytes using acetylthiocholineiodide as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by DTNB reagent based Ellman's method | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | 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. |
| AID1576120 | Neuroprotective activity against amyloid beta (1 to 42)-induced neurotoxicity in Sprague-Dawley rat hippocampal neuron assessed as cell survival rate at 10 uM incubated for 48 hrs in presence of amyloid beta (1 to 42) by CellTiter Glo-based luminescence a | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | The synthesis and biological evaluation of novel gardenamide A derivatives as multifunctional neuroprotective agents. |
| AID1308839 | Non-competitive inhibition of horse serum BuChE using butyrylthiocoline iodide as substrate incubated for 20 mins by Lineweaver-Burk plot analysis | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1756692 | Inhibition of rat serum BuChE using S-butyrylthiocholine iodide as substrate incubated for 8 mins by Ellman's method | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1537663 | Inhibition of human amyloid beta (1 to 42) self-induced aggregation assessed as Amyloid beta (1 to 42) aggregation at 100 uM incubated for 48 hrs by thioflavin T-based fluorescence assay (Rvb = 100%) | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID724167 | Inhibition of butyrylcholinesterase (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase. |
| AID1877970 | Inhibition of human AChE induced amyloid beta (1 to 40 residues) (unknown origin) aggregation at 100 uM relative to control | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease. |
| AID1702420 | Inhibition of human serum BChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1691738 | Antialzheimer activity in AlCl3-induced Zebrafish model of Alzheimer's disease assessed as increase in motility speed at 8 uM relative to control | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1673641 | Displacement of propidium iodide from PAS region of human erythrocytes AChE at 10 uM incubated for 6 hrs by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1453098 | Selectivity index, ratio of IC50 for rat serum BuChE to IC50 for 5% rat cortex homogenate AChE | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease. |
| AID1484839 | Reversal of scopolamine-induced memory impairment in Kunming mouse assessed as step-down latency time at 5 mg/kg, po administered 60 mins prior to training trial followed by scopolamine challenge at 30 mins post dose measured 24 hrs after training trial b | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID48731 | Maximum reversal of vecuronium-induced neuromuscular block in-vivo in anaesthetised cats | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. |
| AID1691734 | Antialzheimer activity in AlCl3-induced Zebrafish model of Alzheimer's disease assessed as change in motility speed at 8 uM (Rvb = 1.08 mm/s) | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1633168 | Inhibition of human BACE1 using as 7-Methoxycoumarin-4-acetyl-[Asn670, Leu671]-Amyloid beta/A4 precursor protein 770 fragment 667-676-(2,4-dinitrophenyl) Lys-Arg-Arg amide trifluoroacetate salt as substrate incubated for 2 hrs by FRET based florescence as | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1359856 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition by Ellman's method | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds. |
| AID1330783 | Hepatotoxicity in scopolamine-induced memory deficit Kunming mouse model assessed as area of necrosis in hepatocytes at 5 mg/Kg, po for 6 days by hematoxylin and eosin-staining based microscopic analysis | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1773275 | Anti-alzheimer activity against oligomerized-amyloid beta (1 to 42) peptide-induced cognitive dysfunction ICR mouse model assessed as reduction in escape latency time at 15 mg/kg, po administered from day 3 to 14 by Morris water maze test | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1633186 | Effect on total arm entries in scopolamine-induced spatial memory impairment in Wistar rat model of amnesia at 5 mg/kg, po administered once daily for 1 week followed by scopolamine challenge 30 mins prior to test by Y-maze test relative to control | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1279136 | Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1756689 | Ex vivo inhibition of AChE in ig dosed ICR mouse hippocampal homogenate using acetylthiocholine iodide as substrate by DTNB reagent based assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1191938 | Inhibition of AChE from rat cortex homogenate using acetylthiocholine iodide as substrate after 15 mins by Ellman method | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Design, synthesis and evaluation of chromone-2-carboxamido-alkylbenzylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1762616 | Neuroprotection against icv infused amyloid beta (1 to 42)-induced ICR mouse model of Alzheimer's disease assessed as rescue of decrease neuronal cells in hippocampal at to 2 mg/kg, po administered daily for 7 days by HE staining | |||
| AID1406144 | Permeability of the compound in pH 7.4 PBS by PAMPA-BBB assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease. |
| AID1416362 | Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1217728 | Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1261780 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as pyknotic nucleus in CA2 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxylin | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID682339 | Inhibition of human erythrocyte AChE using acetylthiocholine as substrate by Ellman method | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: synthesis, biological assessment, and molecular modeling. |
| AID1279143 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1501683 | Binding affinity to electric eel AChE by STD NMR spectroscopy method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID1555977 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1176158 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 0.01 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1322993 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured for 2 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and anticholinesterase activity of coumarin-3-carboxamides bearing tryptamine moiety. |
| AID763834 | Activity at AChE in Charles Foster rat hypothalamus assessed as substrate hydrolyzed per mg of protein at 5 mg/kg, po for 8 days by Ellman's method (Rvb = 40.50 +/- 0.76 mol/min) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1693560 | Inhibition of self-induced human amyloid beta (1 to 42) aggregation at 25 uM incubated for 24 hrs by thioflavin T-based fluorescence assay relative to control | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID1736943 | Inhibition of human serum BChE by Ellman's method | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1906406 | Antialzheimer activity against scopolamine-induced cognitive deficit ICR mouse model assessed as improvement in memory impairment by measuring reduction in number of errors at 5 mg/kg, ig by step-through passive avoidance test | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1533605 | Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate after 10 mins measured for every mins by Ellman's method | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID763835 | Activity at AChE in Charles Foster rat hippocampus assessed as substrate hydrolyzed per mg of protein at 10 mg/kg, po for 8 days by Ellman's method (Rvb = 47.50 +/- 0.84 mol/min) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1517863 | Inhibition of equine butyrylcholinesterase using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID748769 | Selectivity ratio of IC50 for human serum BChE to IC50 for electric eel AChE | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Design, synthesis and evaluation of some new 4-aminopyridine derivatives in learning and memory. |
| AID1254985 | Inhibition of Torpedo californica AChE (type VI-S) using acetylthiocholine iodide as substrate assessed as 5-thio-2-nitrobenzoate anion formation preincubated for 15 mins followed by substrate addition | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Synthesis and structure-activity relationship study of benzofuran-based chalconoids bearing benzylpyridinium moiety as potent acetylcholinesterase inhibitors. |
| AID462783 | Inhibition of human BuChE preincubated for 20 mins before substrate addition by Ellman's method | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238. |
| AID230724 | Ratio of the IC50 values of BuChE and AcHe | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
| AID1884574 | Inhibition of PDE4D7 (unknown origin) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID1877962 | Inhibition of rat serum BuChE by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease. |
| AID1901710 | Toxicity in Sprague-Dawley rat assessed as median lethal dose administered intraperitoneally as single dose | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents. |
| AID311934 | Dissociation constant, pKa of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID282007 | Inhibition of human recombinant AChE | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties. |
| AID1077092 | Inhibition of rat cortex homogenate AchE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1609220 | Improvement in learning and spatial memory in icv infused amyloid beta (1 to 42)-induced Wistar rat model of Alzheimer's disease assessed as increase in number of platform crossing at 5 mg/kg, po administered daily for 7 days starting from 7 days post sur | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1555976 | Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1694230 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured after 4 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Novel arylcarbamate-N-acylhydrazones derivatives as promising BuChE inhibitors: Design, synthesis, molecular modeling and biological evaluation. |
| AID1609489 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives. |
| AID1330762 | Inhibition of self-mediated aggregation of amyloid beta (1 to 42 residues) (unknown origin) at 20 uM incubated for 46 to 48 hrs by Thioflavin T binding assay relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID351916 | Selectivity ratio, IC50 for human serum BChE to IC50 for human recombinant AChE | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors. |
| AID1722437 | Cytotoxicity against human SH-SY5Y cells at 0.001 to 100 uM after 24 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | New coumarin-benzotriazole based hybrid molecules as inhibitors of acetylcholinesterase and amyloid aggregation. |
| AID1191948 | Inhibition of self-mediated aggregation of amyloid beta (1-42) (unknown origin) at 25 uM after 24 hrs by thioflavin T fluorescence-based fluorimetric method | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Design, synthesis and evaluation of chromone-2-carboxamido-alkylbenzylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1533633 | In vivo antioxidant activity in Swiss albino mouse brain assessed as increase in SOD level at 1 mg/kg, ip qd pretreated for 1 hr followed by scopolamine addition measured every 30 secs interval for 2 mins | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
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| AID1368600 | Cognition enhancing effect in albino mouse assessed as reversal of scopolamine-induced memory deficit by measuring reduction in number of mistake at 0.5 mg/kg, ip treated 5 mins post scopolamine challenge by step down passive avoidance test | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1570276 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by spectrophotometric analysis | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships. |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1501304 | Neuroprotective activity against H2O2-induced cell death in human SK-N-MC cells assessed as cell viability at 10 uM preincubated for 2 hrs followed by H2O2 addition and measured after 24 hrs by MTT assay (Rvb = 56%) | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1077085 | Antioxidant activity assessed as trolox equivalent of APPH-induced radical scavenging activity at 1 to 10 uM preincubated for 15 mins followed by AAPH challenge measured every minute for 90 minutes by ORAC fluorescence assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1901716 | Selectivity ratio of IC50 for inhibition of C-terminal 6His-tagged human recombinant BuChE (29 to 602 residues) using butyrylthiocholine iodide as substrate to IC50 for inhibition of C-terminal 6His-tagged human recombinant AChE (32 to 614 residues) expre | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents. |
| AID1397451 | Inhibition of human recombinant AChE using acetylthiocholine as substrate by UV-visible spectrophotometric Ellman's method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors. |
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| AID1494310 | Half life in Sprague-Dawley rat liver microsomes at 100 uM up to 180 mins by HPLC-UV analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID1383667 | Antioxidant activity assessed as DPPH radical scavenging activity at 20 uM after 25 mins | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
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| AID1772613 | Inhibition of human recombinant AChE preincubated for 1 min in presence of DNTB followed by addition of acetylthiocholine iodide substrate and measured after 20 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID1767560 | Neuroprotective activity against amyloid beta (25 to 35)-induced cell damage in human SH-SY5Y cells assessed as neuronal viability at 10 uM measured after 24 hrs in presence of amyloid beta (25 to 35) by MTT assay (Rvb = 68.66 +/- 0.11 %) | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant. |
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| AID1459559 | Inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinolone production using kynuramine as substrate after 20 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1441498 | Increase in acetylcholine level in Wistar rat ventral hippocampus at 1 mg/kg, sc after 4 hrs in presence of 1 mg/kg of memantine administered sc by LC-MS/MS based microdialysis method relative to control | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT |
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| AID1732102 | Inhibition of amyloid beta (1 to 42) (unknown origin) aggregation at 22 uM measured after 24 hrs by Transmission electron microscopy method | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | 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. |
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| AID1694233 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 4 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Novel arylcarbamate-N-acylhydrazones derivatives as promising BuChE inhibitors: Design, synthesis, molecular modeling and biological evaluation. |
| AID1707758 | Inhibition of recombinant human BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1766056 | Inhibition of recombinant equine BChE by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors. |
| AID658004 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 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. |
| AID1292349 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 10 mins by modified Ellman's method | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Biological evaluation of synthetic α,β-unsaturated carbonyl based cyclohexanone derivatives as neuroprotective novel inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID707700 | Inhibition of human recombinant GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1815191 | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate by Ellman's method | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID1707767 | Antiinflammatory activity in LPS-induced human THP-1 cells assessed as reduction in IL6 release at 10 uM peincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by EIA | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1877961 | Inhibition of electric eel AChE by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease. |
| AID1379016 | Inhibition of human serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 180 secs by spectrophotometric analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1815197 | Ratio of IC50 for Inhibition of hERG (unknown origin) expressed in CHO-K1 cells to ratio of IC50 for Inhibition of rat cortex AChE | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID1900711 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID1756691 | Ex vivo inhibition of AChE in ig dosed ICR mouse cortex homogenate using acetylthiocholine iodide as substrate by DTNB reagent based assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1736940 | Selectivity index, ratio of IC50 for inhibition of equine serum BChE to IC50 for inhibition of electric eel AChE | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1351504 | Reversal of SCOP-induced cognitive impairment in Sprague-Dawley rat assessed as reduction in time spent exploring novel object over familiar object at 1 mg/kg, po administered 120 mins before familiarization phase measured for 3 mins post familiarization | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID666573 | Inhibition of electric eel acetylcholine esterase using acetylcholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents. |
| AID1552615 | Effect on total arm entries in scopolamine-induced spatial memory impairment in albino mouse model of amnesia at 5 mg/kg, po administered once daily for 7 days followed by scopolamine challenge for 5 mins prior to test and measured on day 7 by Y-maze test | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1701447 | Anti-VaD activity against UCCAO-induced spatial memory deficient C57BL/6J mouse model assessed as improvement in spatial learning and memory by measuring increased the residence time in the platform area at 1 mg/kg, po administered for 21 days by Morris w | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Rational Design of 2-Chloroadenine Derivatives as Highly Selective Phosphodiesterase 8A Inhibitors. |
| AID1657142 | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells at 10 uM using kynuramine as substrate measured after 30 mins by fluorescence based assay relative to control | 2020 | Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8 | Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. |
| AID395663 | Cognitive enhancing effect against scopolamine-induced acquisition memory deficit in mouse assessed as escape latency at 2 mg/kg, intragastric gavage after 24 hrs by step-down passive avoidance test | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives. |
| AID1532588 | Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes at 1 uM after 60 mins relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
| AID1383679 | Reversal of scopolamine-induced memory deficit in Swiss albino mouse assessed as increase in transfer latency time of retention trial at 10 mg/kg, ip administered once daily for 7 days followed by scopolamine challenge and subsequent training session for | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
| AID1339455 | Cognition enhancement activity in Charles Foster albino rat model of spatial working memory assessed as escape latency at 10 mg/kg, po for administered from day 1 to 10 measured 1 hr post last dose on day 8 by Morris water maze test (Rvb = 16.97 +/- 0.8 s | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID289398 | Neuroprotective effect against beta amyloid protein 1-42 treated human IMR32 cells at 0.1 umol/ml after 48 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | 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. |
| AID1209455 | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID670564 | Inhibition of equine BuChE using butyrylthiocholine iodide as substrate after 5 mins by DTNB method | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14 | Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template. |
| AID1625093 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Highly potent and selective aryl-1,2,3-triazolyl benzylpiperidine inhibitors toward butyrylcholinesterase in Alzheimer's disease. |
| AID1500949 | Passive permeability of the compound at 100 uM after 6 hrs by PAMPA | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Hydroxy-substituted trans-cinnamoyl derivatives as multifunctional tools in the context of Alzheimer's disease. |
| AID670566 | Inhibition of BACE1 | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14 | Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template. |
| AID1635494 | Antioxidant activity in rat primary hippocampal cells assessed as inhibition of Abeta (1 to 42)-induced ROS generation incubated for 2 hrs followed by Abeta (1 to 42) challenge measured after 24 hrs by DCFH-DA staining based analysis | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1324375 | Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 8 mins followed by substrate addition by Ellman's method | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Synthesis and biological evaluation of ranitidine analogs as multiple-target-directed cognitive enhancers for the treatment of Alzheimer's disease. |
| AID1339440 | Inhibition of horse serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1494309 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as metabolic rate constant at 100 uM up to 180 mins by HPLC-UV analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID1290886 | Inhibition of Electrophorus electricus acetylcholinesterase using acetylthiocholine iodide substrate after 15 mins by spectrophotometric method | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease. |
| AID1308845 | Reversible inhibition of electric eel AchE using acetylthiocholine iodide as substrate at 1 uM preincubated for 20 mins followed by 100 fold dilution by Ellman method | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1878001 | Antialzheimer activity against scopolamine-induced cognitive deficit mouse model assessed as decrease in lipid peroxidation at 5.0 mg/kg by step-through passive avoidance test | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease. |
| AID1339444 | Antioxidant activity assessed as H2O2 radical scavenging activity at 10 to 100 ug/ml incubated for 10 mins by UV-Visible spectrophotometric method | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1501308 | Metal chelating activity assessed as inhibition of Cu2+ mediated amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM after 2 hrs by turbidity assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1752609 | Displacement of propidium iodide from the PAS site of human AChE at 50 uM preincubated with enzyme for 6 hrs followed by incubation with propidium iodide and measured after 20 mins by fluorescence analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease. |
| AID1705720 | Inhibition of equine serum BChE at 10 uM using S-butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every minute for 10 mins by DTNB-reagent based Ellman's method relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase. |
| AID1077080 | Inhibition of human erythrocytes AChE-induced amyloid beta (1 to 40) aggregation at 100 uM by thioflavin T fluorescence method | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
| AID1076174 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1773258 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 12.5 to 25 uM incubated for 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID361789 | Inhibition of AchE in rat cortex by Ellman's method | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | 2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity. |
| AID1330791 | Cognitive enhancement activity in scopolamine-induced memory deficit Kunming mouse model assessed as increase in step-through latency time at 5 mg/kg, po treated for 1 hr before training followed by scopolamine challenge 30 mins before training measured 2 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1338117 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation. |
| AID1480939 | Neuroprotective activity against rotenone/oligomycin A-induced mitochondrial oxidative stress in human SH-SY5Y cells assessed as cell survival at 0.3 uM pretreated for 24 hrs followed by rotenone/oligomycin A challenge measured after 24 hrs by MTT assay r | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | 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. |
| AID1389180 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID31036 | In vitro inhibition of human recombinant AChE. | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1698420 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1705721 | Inhibition of electric eel AChE at 1 uM using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every minute for 10 mins by DTNB-reagent based Ellman's method relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase. |
| AID1756690 | Ex vivo inhibition of AChE in ICR mouse hippocampal homogenate at 12 mg/kg, ig using acetylthiocholine iodide as substrate measured after 30 to 60 mins by DTNB reagent based assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1407162 | Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID1184268 | Inhibition of electric eel AChE using acetylthiocholine iodide substrate by Ellman method based spectrophotometry | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Indolinone-based acetylcholinesterase inhibitors: synthesis, biological activity and molecular modeling. |
| AID1609506 | Neuroprotective activity in Swiss albino mouse model of STZ-induced cognition deficit assessed as reduction in Abeta42 deposition level in brain at 5 mg/kg, po administrated for 15 days by ELISA | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives. |
| AID1339452 | Cognition enhancement activity in Charles Foster albino rat model of spatial working memory assessed as escape latency at 10 mg/kg, po for administered from day 1 to 10 measured 1 hr post last dose on day 7 by Morris water maze test (Rvb = 17.45 +/- 0.62 | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1773276 | Anti-alzheimer activity against oligomerized-amyloid beta (1 to 42) peptide-induced cognitive dysfunction ICR mouse model assessed as reduction in amyloid beta (1 to 42) peptide level in brain at 15 mg/kg, po administered from day 3 to 14 by ELISA | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1633198 | Antioxidant activity Wistar rat model of scopolamine-induced amnesia assessed as reduction in MDA levels in brain homogenates at 5 mg/kg, po by TBARS assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1385849 | Reversal of scopolamine-induced cognitive impairment in Wistar Hannover rat assessed as improvement in episodic memory at 1.8 mg/kg, ip administered 30 mins prior to testing by novel object recognition test | 2018 | ACS medicinal chemistry letters, Aug-09, Volume: 9, Issue:8 | Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor. |
| AID1055867 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 15 mins prior to substrate addition by Ellman's method | 2013 | European journal of medicinal chemistry, , Volume: 70 | Novel coumarin-3-carboxamides bearing N-benzylpiperidine moiety as potent acetylcholinesterase inhibitors. |
| AID1480845 | Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID262755 | Anticholinesterase activity against human plasma BChE | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
| AID1826351 | Inhibition of human recombinant MAO-A expressed in supersomes assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate by spectrofluorimetric analysis | |||
| AID1752606 | Displacement of propidium iodide from the PAS site of human AChE at 5 uM preincubated with enzyme for 6 hrs followed by incubation with propidium iodide and measured after 20 mins by fluorescence analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease. |
| AID1609228 | Improvement in learning and spatial memory in icv infused amyloid beta (1 to 42)-induced Wistar rat model of Alzheimer's disease assessed as reduction in disordered neuron in hippocampal region at 5 mg/kg, po administered daily for 7 days starting from 7 | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1347975 | Cytotoxicity against E17 Sprague-Dawley rat primary cortical neurons at 10 to 30 uM after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1201546 | Inhibition of human erythrocyte AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate by Ellman' method | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Novel multitarget-directed ligands (MTDLs) with acetylcholinesterase (AChE) inhibitory and serotonergic subtype 4 receptor (5-HT4R) agonist activities as potential agents against Alzheimer's disease: the design of donecopride. |
| AID1407198 | Half life in Sprague-Dawley rat liver microsomes in presence of NADPH by UPLC/MS analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID763832 | Cognitive enhancing effect in Wistar rat assessed as reversal of learning impairment measured as transfer latency at 5 mg/kg, po for 8 days measured on first day of test by elevated plus maze test (Rvb = 70.846 +/- 0.76 seconds) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1732097 | Inhibition of AChE in human erythrocytes assessed as inhibition of AChE-induced amyloid beta(1 to 42) aggregation at Abeta42:compound concentration ratio of 10:5 measured after 48 hrs by thioflavin-T assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | 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. |
| AID1678497 | Permeability of the compound on PBS buffer pH 7.4 at 100 uM by PAMPA-BBB assay | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12 | α-Linolenic Acid-Valproic Acid Conjugates: Toward Single-Molecule Polypharmacology for Multiple Sclerosis. |
| AID482853 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
| AID1597704 | Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | 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. |
| AID1702502 | Antialzheimer activity against 3 dpf zebrafish model of AlCl3-induced AD assessed as efficacy on speed change at 8 uM relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1478773 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 6 mins followed by substrate addition measured up to 180 sec by Ellman's method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. |
| AID1820985 | Anti-neuroinflammation in mouse BV-2 cells assessed as decrease in LPS-induced iNOS activity at 1.25 umol/L by fluorescence based assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1379216 | Inhibition of electric eel AchE-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by ThT-based fluorescence method relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID31171 | In vitro inhibition of acetylcholinesterase from human erythrocytes | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. |
| AID1605561 | Anti-VaD activity against UCCAO-induced spatial memory deficient C57BL/6J mouse model assessed as improvement in spatial learning and memory by measuring increase in residence time on the platform at 0.7 mg/kg, po administered for 21 days by Morris water | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia. |
| AID1378351 | Inhibition of human AChE using acetylthiocholine as substrate by Ellman's method | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates. |
| AID242428 | In vitro inhibitory concentration against rat cortex acetylcholinesterase | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors. |
| AID1865110 | Anti-neuroinflammatory activity in Abeta42 induced zebrafish AD model assessed as reduction in number of activated microglia relative to control | |||
| AID1831854 | Effective permeability of compound in PBS at pH 7.4 incubated upto 6 hrs by HPLC-MS analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| AID345207 | Inhibition of human recombinant AChE-induced amyloid beta (1-40) aggregation at 100 uM by thioflavin T formation assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer. |
| AID289393 | Selectivity for Electrophorus electricus AChE over human BchE | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | 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. |
| AID1609064 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Discovery of δ-sultone-fused pyrazoles for treating Alzheimer's disease: Design, synthesis, biological evaluation and SAR studies. |
| AID1867627 | Inhibition of human BuChE by Ellman's spectrophotometric method | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease. |
| AID1757186 | Selectivity index, ratio of IC50 for rat serum butyrylcholinesterase to IC50 for rat cortex acetylcholinesterase | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease. |
| AID1055212 | Glutathione peroxidase-like activity of the compound in potassium phosphate buffer assessed as GSH-mediated reduction of H2O2 measured for 10 secs by spectrophotometric analysis (Rvb = 49.5 +/- 2.6 uM/min) | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID1334736 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties. |
| AID1484831 | Metal chelating activity assessed as inhibition of Cu2+ induced amyloid beta (1 to 42) aggregation at 25 uM after 24 hrs by ThT-based fluorometric method relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1335934 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-5 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1705719 | Inhibition of equine serum BChE at 1 uM using S-butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every minute for 10 mins by DTNB-reagent based Ellman's method relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase. |
| AID361790 | Inhibition of BuchE in rat serum by Ellman's method | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | 2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity. |
| AID1379012 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1330765 | Antioxidant activity assessed as AAPH radical scavenging activity by measuring ORAC-FL value at 1 to 10 uM preincubated for 15 mins followed by AAPH radical addition measured every minute for 120 mins by fluorescence method relative to control trolox | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1076769 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 10 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 24 | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1152935 | Hepatotoxicity in human HepG2 cells assessed as cell viability at 30 uM by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1557015 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel N-benzylpiperidine carboxamide derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1635483 | Inhibition of human erythrocyte AChE using ATCI as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1773256 | Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1162589 | Inhibition of human recombinant AChE using acetylthiocholine iodide substrate incubated for 15 mins by spectrophotometry based Ellman's method | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | 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. |
| AID1738184 | Inhibition of HFIP-pretreated human amyloid beta (1 to 42) self aggregation at 10 uM incubated for 36 to 48 hrs by thioflavin-T based fluorescence method relative to control | |||
| AID1694873 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE by Ellman's method | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1176154 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins at 100 uM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1353358 | Inhibition of AChE (unknown origin) | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1597702 | Inhibition of equine serum BChE using butyrylthiocholine as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | 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. |
| AID1736868 | Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | 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. |
| AID1711761 | Inhibition of electric eel AchE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Development of cyanopyridine-triazine hybrids as lead multitarget anti-Alzheimer agents. |
| AID1698421 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation assessed as normalized fluorescence intensity at 5 to 20 uM by Thioflavin T based fluorometric assay relative to control | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1407184 | Inhibition of AChE-induced amyloid beta 40 (unknown origin) aggregation at 100 uM by thioflavin-T fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID725915 | Inhibition of AChE (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors. |
| AID1126626 | Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 10 mins before substrate addition after 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | 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. |
| AID1700047 | Inhibition of human erythrocytes AChE by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation. |
| AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
| AID1261766 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as condensed cytoplasm in CA2 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxyl | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1444087 | Antioxidant activity assessed as inhibition of AAPH-induced peroxyl radical generation measured as trolox equivalent at 1 to 10 uM preincubated for 15 mins followed by AAPH addition measured every minute for 90 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1702498 | Antialzheimer activity against 3 dpf zebrafish model of AlCl3-induced AD assessed as motility by measuring change in speed at 8 uM (Rvb = 1.05 mm/s) | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID695008 | Antialzheimer activity in Kunming mouse assessed as reversal of amyloid beta (1 to 42)-induced impairments in spartial recognition memory at 0.65 mg/kg, po qd measured on day 3 and 4 by morris water maze test | 2012 | ACS medicinal chemistry letters, Nov-08, Volume: 3, Issue:11 | Identification of aminopyridazine-derived antineuroinflammatory agents effective in an Alzheimer's mouse model. |
| AID707698 | Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1360317 | Inhibition of Torpedo californica AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and β-secretase inhibition activities. |
| AID1383663 | Inhibition of electric eel AChE-induced amyloid beta (1 to 42) aggregation at 0.5 uM after 48 hrs by thioflavin T fluorescence spectroscopic method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
| AID454342 | Inhibition of AChE in rat cortex after 15 mins by modified Ellman's method | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors. |
| AID1568795 | Antioxidant activity assessed as trolox equivalents of AAPH radical scavenging activity preincubated for 15 mins followed by AAPH addition and measured every minute for 90 mins by ORAC-FL assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID31023 | Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in human erythrocytes | 1998 | Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6 | Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase. |
| AID30678 | Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in bovine brain | 1998 | Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6 | Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase. |
| AID1879288 | Inhibition of equine serum BuChE | 2022 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 61 | 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. |
| AID635877 | Inhibition of rat liver mitochondrial MAO-A using [14C]-5-hydroxytryptamine after 30 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | 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 di |
| AID1784743 | Inhibition of equine serum BuChE using butyrylthiocholine as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT |
| AID1704850 | Memory enhancement effect in dizocilpine-induced Wistar (Krf:WI) rat model of amnesia assessed as decrease in transfer latency time at 1 mg/kg, ip measured after 30 to 45 mins by elevated plus maze test | |||
| AID1533627 | In vivo antioxidant activity activity in Swiss albino mouse brain assessed as increase in catalase activity by measuring decrease in H2O2 level at 1 mg/kg, ip qd pretreated for 1 hr followed by scopolamine addition | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1609066 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Discovery of δ-sultone-fused pyrazoles for treating Alzheimer's disease: Design, synthesis, biological evaluation and SAR studies. |
| AID1633203 | Inhibition of mouse plasma BuChE using S-butyrylacetylthiocholine iodide as substrate at 10 uM measured after 30 mins by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1279144 | Selectivity index, ratio of human serum BuChE to IC50 for human erythrocyte AChE | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1738110 | Displacement of propidium iodide from human AChE at 50 uM incubated for 6 hrs followed by propidium iodide addition and measured after 20 mins by fluorescence based assay relative to control | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1176156 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins at 500 uM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1711763 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Development of cyanopyridine-triazine hybrids as lead multitarget anti-Alzheimer agents. |
| AID1329701 | Inhibition of butyrylcholinesterase (unknown origin) using butyrylthiocholine chloride as substrate incubated for 10 mins followed by substrate addition measured after 20 mins by UV-Vis spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1 | Synthesis, structure-activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID1884595 | In vivo inhibition of AChE in hippocampus of aggregated Abeta(25-35)-induced Alzheimer's disease C57BL/6 mouse model at 1 mg/kg, iv measured after 2 hrs in presence of 1 mg/kg, iv rolipram by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID1347793 | Inhibition of amyloid beta (25 to 35 residues) (unknown origin)-induced toxicity in rat PC12 cells assessed as protection against amyloid beta (25 to 35 residues)-induced apoptosis by measuring viable cells at 50 ug/ml by Annexin V-FITC/propidium iodide s | |||
| AID1655646 | Mixed type inhibition of human AChE using acetylthiocholineiodide as substrate measured for every 30 sec for 5 mins by Ellman's method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor. |
| AID1866876 | Inhibition of Electrophorus electricus AchE using acetylcholine iodide as substrate incubated for 10 mins followed by substrate addition measured at 0 to 180 secs by Ellman's method | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors. |
| AID1261765 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as condensed cytoplasm in CA3 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxyl | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1901714 | Inhibition of C-terminal 6His-tagged human recombinant AChE (32 to 614 residues) expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents. |
| AID1657140 | Inhibition of HFIP-pretreated self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM measured after 24 hrs by ThT fluorescence assay relative to control | 2020 | Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8 | Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. |
| AID1906404 | In vivo inhibition of AChE in ICR mouse hippocampus using acetylthiocholine iodide as substrate at 10 mg/kg, ig measured after 1 hr by microplate reader analysis | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1384013 | Effective permeability of the compound dissolved in PBS containing 1% F-127 at 100 uM after 3 to 6 hrs by PAMPA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
| AID1609490 | Cognitive enhancing effect in Swiss albino mouse model of STZ-induced cognition deficit assessed as increase in time spent in target quadrant at 5 mg/kg, po administrated for 15 days and measured at 5th day of training session for 60 secs by Morris water | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives. |
| AID1217710 | Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1784499 | Inhibition of tau aggregation (unknown origin) in Escherichia coli BL21 (DE3) at 10 uM incubated overnight by thioflavin S based fluorescence analysis relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | 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. |
| AID1557018 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel N-benzylpiperidine carboxamide derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1738107 | Displacement of propidium iodide from human AChE at 5 uM incubated for 6 hrs followed by propidium iodide addition and measured after 20 mins by fluorescence based assay relative to control | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1533609 | Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM after 30 mins under dark condition relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1257001 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins by Ellman's method | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease. |
| AID1650984 | Inhibition of equine serum BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents. |
| AID289397 | Inhibition of Electrophorus electricus AchE-induced beta amyloid protein 1-42 co-aggregation at 1 uM by thioflavin T assay | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | 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. |
| AID1738135 | Ex vivo antioxidant activity in brain of scopolamine-induced Swiss albino mouse model of amnesia assessed as increase in SOD level at 5 mg/kg, po administered for 7 days and observed after 30 mins before scopolamine treatment and measured after 15 mins | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1581645 | Inhibition of recombinant human BACE1 using Rh-EVNLDAEFK-Quencher as substrate measured after 60 mins by FRET based spectrofluorometric assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | 1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease. |
| AID1879291 | Inhibition of BuchE (unknown origin) at 10 uM relative to control | 2022 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 61 | 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. |
| AID1207739 | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits | 2013 | Scientific reports, , Volume: 3 | MICE models: superior to the HERG model in predicting Torsade de Pointes. |
| AID1378864 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1736951 | Inhibition of Cu2+-induced amyloid beta (1 to 42 residues) (unknown origin) aggregation at 25 uM after 24 hrs by thioflavin-T fluorescence method relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID1444078 | Inhibition of BuChE in human serum using butyrylthiocholine chloride as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1309432 | Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity preincubated for 15 mins followed by AAPH challenge measured every min for 80 mins by ORAC-FL assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Design, synthesis and evaluation of novel indandione derivatives as multifunctional agents with cholinesterase inhibition, anti-β-amyloid aggregation, antioxidant and neuroprotection properties against Alzheimer's disease. |
| AID1553354 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins under dark condition by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18 | Microwave-Assisted Organic Synthesis, structure-activity relationship, kinetics and molecular docking studies of non-cytotoxic benzamide derivatives as selective butyrylcholinesterase inhibitors. |
| AID1693559 | Inhibition of human BChE using butyrylthiocholineiodide as substrate incubated for 10 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID1702430 | Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at 0.1 times IC50 measured at 120 mins using diluted compound relative to basal level | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1906365 | Inhibition of AChE in mouse cerebral cortex using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 180 secs by Ellman's spectrophotometric method | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1578229 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Search for new multi-target compounds against Alzheimer's disease among histamine H |
| AID1555978 | Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM incubated for 2 hrs under dark condition relative to control | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1532589 | Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
| AID748770 | Inhibition of human serum BChE using butyrylthiolcholine iodide as substrate incubated for 20 mins prior to substrate addition by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Design, synthesis and evaluation of some new 4-aminopyridine derivatives in learning and memory. |
| AID1453100 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate after 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease. |
| AID1633215 | Antiinflammatory activity in mouse BV2 cells assessed as reduction in LPS-induced IL-6 production at 10 uM pretreated for 1 hr followed by LPS challenge and measured after 24 hrs by ELISA assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1201372 | Inhibition of equine serum butyrylcholine esterase incubated for 15 mins using S-butyrylthiocholine chloride substrate by colorimetric Ellman's method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Blood-brain barrier permeable anticholinesterase aurones: synthesis, structure-activity relationship, and drug-like properties. |
| AID724165 | Inhibition of equine butyrylcholinesterase using butyrylthiocholine as substrate incubated for 20 mins prior to substrate addition measured after 3 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase. |
| AID1773257 | Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1484816 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1635491 | Neuroprotective activity against H2O2-induced oxidative damage in human SH-SY5Y cells assessed as increase in cell viability at 20 uM incubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1076768 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 10 nM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rela | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1585836 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID282010 | Antagonist activity at muscarinic M2 receptor assessed as contraction of electrically stimulated guinea pig left atrium at 10 uM | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties. |
| AID1698431 | Ex vivo inhibition of AChE in brain of scopolamine-induced Wistar rat model of amnesia at 5 mg/kg, po pretreated for 7 days followed by scopolamine challenge using acetylthiocholine iodide as substrate by Ellman's method | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1820953 | Inhibition of amyloid beta (1 to 42 ) (unknown origin) aggregation at 20 umol/L incubated for 24 hrs by thioflavin-T fluorescence method relative to control | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1167542 | Selectivity ratio of IC50 for equine BChE to IC50 for electric eel AChE | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1882052 | Inhibition of recombinant bovine mitochondrial MAO-A using benzylamine or serotonin as substrate incubated for 60 mins by fluorimetry assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID1334755 | Inhibition of rat serum BuChE measured after 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties. |
| AID1707766 | Antiinflammatory activity in LPS-induced human THP-1 cells assessed as reduction in IL1beta release at 10 uM peincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by EIA | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1820980 | Anti-neuroinflammation in mouse BV-2 cells assessed as decrease in LPS-induced IL-6 production at 1.25 umol/L measured after 24 hrs by ELISA | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID682359 | Selectivity index, ratio of IC50 for human serum BChE to IC50 for human erythrocyte AChE | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: synthesis, biological assessment, and molecular modeling. |
| AID1261754 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as irregular shape in CA3 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxylin a | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1176157 | Inhibition of human recombinant CYP3A4 expressed in insect cell microsomes preincubated for 10 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1506845 | Antioxidant activity assessed as trolox equivalents of AAPH radical scavenging activity at 0.5 to 10 uM preincubated for 15 mins followed by AAPH addition measured every 60 sec for 120 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Rational design, synthesis and biological screening of triazine-triazolopyrimidine hybrids as multitarget anti-Alzheimer agents. |
| AID1557016 | Inhibition of BuChE in equine serum using Butyrylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Novel N-benzylpiperidine carboxamide derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1824588 | Metabolic stability in CD-1 mouse liver microsomes assessed as half life measured upto 45 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1533624 | Neurotoxicity in Swiss albino mouse assessed as motor coordination by measuring fall off time at 5 mg/kg, po after 1 hr by rota rod test (Rvb = 310.61 +/- 26.64 sec) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1480847 | Inhibition of human serum BuChE using butylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1253473 | Inhibition of electric eel AChE using thiocholine iodide as substrate by Ellman's method | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors. |
| AID1657147 | Antialzheimer activity in scopolamine-induced Kunming mouse model of memory impairment assessed as decrease in number of electric shock at 5 mg/kg/day, ig for 7 days followed by training trial at 1 hr post dose on day 6 and subsequent scopolamine challeng | 2020 | Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8 | Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. |
| AID1293942 | Inhibition of electric eel AChE preincubated for 15 mins followed by addition of acetylthiocholine iodide substrate by Ellman's method-based spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9 | Design, synthesis and bioactivity of novel phthalimide derivatives as acetylcholinesterase inhibitors. |
| AID1532590 | Inhibition of human erythrocytes AChE at 1 uM using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min time interval for 10 mins by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
| AID1701452 | Anti-VaD activity against UCCAO-induced spatial memory deficient C57BL/6J mouse model assessed as improvement in spatial learning and memory by measuring decrease in error rate at 1 mg/kg, po administered for 21 days by passive avoidance test | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Rational Design of 2-Chloroadenine Derivatives as Highly Selective Phosphodiesterase 8A Inhibitors. |
| AID1191949 | Inhibition of Cu2+-mediated aggregation of amyloid beta (1-42) (unknown origin) at 25 uM after 24 hrs by thioflavin T fluorescence-based fluorimetric method | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Design, synthesis and evaluation of chromone-2-carboxamido-alkylbenzylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1673652 | Improvement in learning and spatial memory in icv infused amyloid beta (1 to 42)-induced rat model of Alzheimer's disease assessed as reduction in escape latency at 5 mg/kg, po administered daily for 7 days starting from 7 days post surgery and measured d | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1906378 | Antioxidant activity against okadaic acid-induced ROS generation in human SH-SY5Y cells assessed as reduction in DCF fluorescence intensity at 5 uM pretreated for 24 hrs followed by okadaic acid addition for 24 hrs by DCFH-DA dye based fluorescence analys | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID763831 | Cognitive enhancing effect in Wistar rat assessed as reversal of learning impairment measured as transfer latency at 10 mg/kg, po for 8 days measured on first day of test by elevated plus maze test (Rvb = 70.846 +/- 0.76 seconds) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1609503 | Cognitive enhancing effect in Swiss albino mouse model of STZ-induced cognition deficit assessed as increase in spontaneous alteration at 5 mg/kg, po administrated for 15 days and measured for 8 mins by Y-maze test | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives. |
| AID1854650 | In vivo antagonist activity at 5-HT6R in Sprague-Dawley rat assessed as increase in intracerebral hippocampal acetylcholine level at 1 mg/kg, ip measured every 20 mins for 360 mins by LC-MS/MS analysis relative to control | |||
| AID1533621 | Memory enhancing effect in Swiss albino mouse assessed as reversal of scopolamine-induced reduction in latency time at 1 mg/kg, ip qd pretreated for 1 hr followed by scopolamine addition by passive avoidance test | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1077075 | Cognition enhancing effect against scopolamine-induced memory deficit in Kunming mouse assessed as increase in latency time at 5 mg/kg, po administered 1 hr before training followed by scopolamine challenge for 7 days measured after 24 hrs by step-down pa | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1771808 | Inhibition of equine serum BuChE using BTC as substrate preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT |
| AID1632233 | Antiamnesic activity in Albino LACA mouse assessed as scopolamine-induced increase in escape latency time at 1 mg/kg, ip administered 5 mins post scopolamine challenge for 35 mins by Morris water maze test (Rvb = 49.35 +/- 2.21 secs) | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19 | Coumarin derivatives as potential inhibitors of acetylcholinesterase: Synthesis, molecular docking and biological studies. |
| AID1379015 | Inhibition of human erythrocytic AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 180 secs by spectrophotometric analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1152936 | Hepatotoxicity in human HepG2 cells assessed as cell viability at 100 uM by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID771354 | Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Design, synthesis, biological evaluation and docking study of 5-oxo-4,5-dihydropyrano[3,2-c]chromene derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID1722425 | Inhibition of equine serum BuChE by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | New coumarin-benzotriazole based hybrid molecules as inhibitors of acetylcholinesterase and amyloid aggregation. |
| AID1430427 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 5 mins by spectrophotometry based Ellman method | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | 3,4-Dihydroquinazoline derivatives inhibit the activities of cholinesterase enzymes. |
| AID1347798 | Inhibition of amyloid beta (25 to 35 residues) (unknown origin)-induced toxicity in rat PC12 cells assessed as cell survival at 50 ug/ml after 1 to 3 weeks by clonogenic assay (Rvb = 25%) | |||
| AID1889348 | Reversible inhibition of human AChE assessed as increase in enzyme activity at 0.1 times of IC50 concentration by dilution method relative to control | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1718166 | Inhibition of [3H]DTG binding to sigma 1 receptor (unknown origin) | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases. |
| AID600979 | Inhibition of human plasma AChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID1698412 | Inhibition of human BChE by Ellman's method | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1555975 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1290889 | Antioxidant activity assessed as AAPH scavenging activity assessed as trolox equivalent after 15 mins measured every min for 90 mins by ORAC-FL method relative to control trolox | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease. |
| AID1515408 | Acute toxicity in iv dosed Swiss mouse | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2 | In silico, NMR and pharmacological evaluation of an hydroxyoxindole cholinesterase inhibitor. |
| AID1820949 | Reversible inhibition of electric eel AChE assessed as residual enzyme activity using acetylthiocholine iodide as substrate at 0.1 times IC50 incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID595292 | Inhibition of human AChE-induced beta-amyloid (1-40) aggregation at 100 uM by thioflavin-T based fluorimetric assay | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1633212 | Neuroprotective activity against copper-induced cytotoxicity in human SH-SY5Y cells expressing APP Swedish mutant assessed as increase in cell viability at 10 uM pre-incubated for 2 hrs followed by copper addition and measured after 24 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1707754 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1311914 | Inhibition of electric eel ACHE preincubated for 6 mins followed by addition of acetylcholine iodide as substrate by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1347789 | Inhibition of amyloid beta (25 to 35 residues) (unknown origin)-induced toxicity in rat PC12 cells assessed as increase in cell viability at 50 ug/ml preincubated for 2 hrs followed by amyloid beta (25 to 35 residues) addition measured after 24 hrs by MTT | |||
| AID1152933 | Hepatotoxicity in human HepG2 cells assessed as cell viability at 3 uM by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1809143 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 to 20 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, synthesis, and cholinesterase inhibition assay of liquiritigenin derivatives as anti-Alzheimer's activity. |
| AID1702424 | Pseudo-irreversible inhibition of human erythrocytes AChE assessed as enzyme recovery activity at IC50 using undiluted compound relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1756687 | Ex vivo inhibition of AChE in ICR mouse cortex homogenate at 12 mg/kg, ig using acetylthiocholine iodide as substrate measured after 30 to 180 mins by DTNB reagent based assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1444073 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1335936 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-7 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1818853 | Cognitive enhancing effect in Wistar rat model of scopolamine-induced short term memory impairment assessed as increase in spontaneous alteration at 5 mg/kg measured by Y-maze method | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Designed Peptide Inhibitors of STEP Phosphatase-GluA2 AMPA Receptor Interaction Enhance the Cognitive Performance in Rats. |
| AID1360318 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and β-secretase inhibition activities. |
| AID1884578 | Inhibition of horse serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 10 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID1322906 | Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation. |
| AID1569979 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID594821 | Inhibition of BChE | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | (+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase. |
| AID1339464 | Antioxidant activity in Charles Foster albino rat assessed as reduction in aspartame-induced GSH depletion in brain by measuring GSH level per mg of protein at 10 mg/kg, po by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1152945 | Protein binding in plasma (unknown origin) | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1609498 | Memory enhancement effect in Swiss albino mouse model of STZ-induced cognition deficit assessed as increase in exploratory preference at 5 mg/kg, po administrated for 15 days and measured for 5 mins by novel object recognition test | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives. |
| AID1530636 | Neuroprotection against rotenone/H2O2-induced cell death in human SH-SY5Y cells assessed as increase in cell viability at 0.1 to 2.5 uM preincubated for 24 hrs followed by rotenone/H2O2 addition measured after 24 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Investigating alkyl nitrates as nitric oxide releasing precursors of multitarget acetylcholinesterase-monoamine oxidase B inhibitors. |
| AID1339451 | Cognition enhancement activity in Charles Foster albino rat model of spatial reference memory assessed as increase in time spent in target quadrant during probe trial at 10 mg/kg, po for 4 days administered from day 1 to 4 measured 1 hr post last dose on | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID289395 | Inhibition of beta amyloid protein 1-42 aggregation by thioflavin T assay | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | 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. |
| AID1261744 | Cognitive enhancing effect in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as swimming path length in effective region at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by Morris water ma | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1810376 | Inhibition of human recombinant GSK-3beta using prephosphorylated polypeptide as substrate incubated for 30 mins in presence of ATP by Kinase-Glo luminescence assay | |||
| AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1359867 | Neuroprotection against H2O2-induced cell death in human SH-SY5Y cells assessed as cell viability at 100 uM preincubated for 3 hrs followed by H2O2 addition measured after 24 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds. |
| AID1184270 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Indolinone-based acetylcholinesterase inhibitors: synthesis, biological activity and molecular modeling. |
| AID1569986 | Reversible inhibition of equine serum BuChE assessed as enzyme activity at 0.1xIC50 using butyrylthiocholine iodide as substrate measured at 240 mins after dilution by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1225715 | Reversal of scopolamine-induced cognitive deficit in Kunming mouse assessed as longer latency time at 5 mg/kg, po administered 1 hr before training trial measured at 24 hrs after training trial by passive avoidance test | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1308841 | Selectivity ratio of IC50 for horse serum BuChE to IC50 for human erythrocytes AchE | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1707760 | Inhibition of equine serum BChE at 10 uM using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 10 mins by Ellman's method relative to control | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1520013 | Half life in rat liver microsomes up to 60 mins by HPLC-LC/MS analysis | |||
| AID1261768 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as reduction of dead neurons in CA1 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hem | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1152941 | Effective permeability across human intestinal membrane by Ussing chamber technique | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1220557 | Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
| AID32285 | Inhibitory concentration required against acetylcholinesterase activity | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Synthesis and screening for antiacetylcholinesterase activity of (1-benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles related to donepezil. |
| AID384081 | Inhibition of rat plasma butyrylcholine esterase in presence of butyrylcholine substrate by chemiluminescent assay | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID1773260 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1421883 | Inhibition of human serum BuChE using butyrylthiocholine as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors. |
| AID1397453 | Inhibition of horse serum BuChE using acetylthiocholine as substrate by UV-visible spectrophotometric Ellman's method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors. |
| AID1152938 | Hepatotoxicity in human HepG2 cells assessed as cell viability at 1000 uM by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1397457 | Effective permeability of the compound at 100 ug/ml after 16 hrs by PAMPA | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors. |
| AID1217707 | Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1384014 | Effective permeability of the compound dissolved in PBS at 100 uM after 3 to 6 hrs by PAMPA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
| AID1766053 | Inhibition of recombinant human AChE expressed in HEK293 cells by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors. |
| AID1416368 | Selectivity index, ratio of IC50 for human serum BuChE to IC50 for human erythrocytes AChE | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1427876 | Cytotoxicity against human SH-SY5Y cells after 72 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Targeting Alzheimer's disease by investigating previously unexplored chemical space surrounding the cholinesterase inhibitor donepezil. |
| AID1339443 | Antioxidant activity assessed as DPPH radical scavenging activity at 10 to 100 ug/ml incubated for 30 mins under dark condition | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1308840 | Selectivity ratio of Ki for horse serum BuChE to Ki for human erythrocytes AchE | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors. |
| AID1884596 | Anti-neuroinflammatory activity against aggregated Abeta(25-35)-induced Alzheimer's disease C57BL/6 mouse model assessed as inhibition of TNF-alpha production in hippocampus at 1 mg/kg, iv measured after 2 hrs in presence of 1 mg/kg, iv rolipram by ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID1217727 | Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1473875 | Ratio of drug concentration at steady state in human at 5 to 10 mg, po after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1635511 | Antiapoptotic activity in Wistar rat brain hippocampus assessed as attenuation of Abeta (1 to 42) insult-induced increase in cleaved caspase-3 expression level at 5 mg/kg, po administered for 15 days by Western blot analysis | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1501657 | Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by UV-Vis spectrophotometric analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID1906408 | Inhibition of AChE in human SH-SY5Y differentiated neuronal cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser396 residue at 0.001 to 5 uM by ELISA | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1707550 | Drug concentration in wild type C57BL6 mouse brain at 2 mg/kg, ip thrice a week for 2 weeks observed after 4 hrs post last dose by HPLC/MS/MS analysis | |||
| AID1443228 | Selectivity for acetylcholinesterase (unknown origin) over butyrylcholinesterase (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Green synthesis of novel spiro-indenoquinoxaline derivatives and their cholinesterases inhibition activity. |
| AID1501300 | Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1756684 | Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as on rate constant at 298.15 K by surface plasmon resonance assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID538478 | Inhibition of human acetyl cholinesterase by Ellmann's method | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23 | Substituted spiro [2.3'] oxindolespiro [3.2″]-5,6-dimethoxy-indane-1″-one-pyrrolidine analogue as inhibitors of acetylcholinesterase. |
| AID1826354 | Inhibition of horse serum BChE by Ellman's spectrophotometric assay | |||
| AID1184269 | Inhibition of equine serum BuChE using butyrylthiocholine iodide substrate by Ellman method based spectrophotometry | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Indolinone-based acetylcholinesterase inhibitors: synthesis, biological activity and molecular modeling. |
| AID1564981 | Inhibition of human erythrocytes AChE assessed as reduction in 5-thio-2-nitrobenzoate anion formation at 10'-6 M using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Novel multi target-directed ligands targeting 5-HT |
| AID1701446 | Anti-VaD activity against UCCAO-induced spatial memory deficient C57BL/6J mouse model assessed as improvement in spatial learning and memory by measuring reduction in escape latency at 1 mg/kg, po administered for 21 days by Morris water maze test | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Rational Design of 2-Chloroadenine Derivatives as Highly Selective Phosphodiesterase 8A Inhibitors. |
| AID1217708 | Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID31010 | In vitro inhibition of Torpedo californica acetylcholinesterase. | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | Aminopyridazines as acetylcholinesterase inhibitors. |
| AID1737037 | Antialzheimer activity in Alcl3-induced zebra fish AD model assessed as increase in motility at 8 uM relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID314093 | Inhibition of human AchE-induced amyloid beta aggregation at 100 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Multi-target-directed ligands to combat neurodegenerative diseases. |
| AID1309430 | Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM incubated for 48 hrs measured after 5 mins by thioflavin-T fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Design, synthesis and evaluation of novel indandione derivatives as multifunctional agents with cholinesterase inhibition, anti-β-amyloid aggregation, antioxidant and neuroprotection properties against Alzheimer's disease. |
| AID1674780 | Inhibition of AChE in rat brain using acetylthiocholine iodide as substrate by Ellman's UV-vis spectrophotometric method | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18 | Synthesis and biological evaluation of novel quinazoline-triazole hybrid compounds with potential use in Alzheimer's disease. |
| AID1702433 | Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM by ThT fluorescence assay relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1533612 | Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1176166 | Absolute bioavailability in dog | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1757180 | Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation by T-fluorescence assay relative to control | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease. |
| AID1552594 | Inhibition of human erythrocyte AChE-induced amyloid beta (1 to 42) (unknown origin) aggregation at 5 uM to 20 uM incubated for 48 hrs by fluorescence based thioflavin T assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1625094 | Inhibition of recombinant human BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Highly potent and selective aryl-1,2,3-triazolyl benzylpiperidine inhibitors toward butyrylcholinesterase in Alzheimer's disease. |
| AID1338119 | Inhibition of recombinant human BACE1 expressed in baculovirus expression system at 50 uM using Rh-EVNLDAEFK-quencher as substrate after 60 mins by spectrofluorometric method relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation. |
| AID677026 | Antiamnesic activity in scopolamine-induced amnesia mouse model assessed as increase in time spent in target quadrant at 25 mg/kg, ip measured on day 5 by Morris water maze test | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis and evaluation of novel 4-[(3H,3aH,6aH)-3-phenyl)-4,6-dioxo-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazol-5(3H,6H,6aH)-yl]benzoic acid derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1576118 | Neuroprotective activity against amyloid beta (1 to 42)-induced neurotoxicity in Sprague-Dawley rat hippocampal neuron assessed as cell survival rate at 0.1 uM incubated for 48 hrs in presence of amyloid beta (1 to 42) by CellTiter Glo-based luminescence | 2019 | MedChemComm, Jul-01, Volume: 10, Issue:7 | The synthesis and biological evaluation of novel gardenamide A derivatives as multifunctional neuroprotective agents. |
| AID1433724 | Cognition enhancing effect in scopolamine-induced cognitive impairment mouse model assessed as increase in time spent in target quadrant at 3 mg/kg, ig administered once in a day for 14 consecutive days followed by scopolamine challenge 1 hr post last dos | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3 | Synthesis and SAR study of novel sarsasapogenin derivatives as potent neuroprotective agents and NO production inhibitors. |
| AID1882050 | Inhibition of BuChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID1702427 | Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at IC50 using undiluted compound relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1738129 | Ex vivo inhibition of AChE in brain of scopolamine-induced Swiss albino mouse model of amnesia at 5 mg/kg, po administered for 7 days and observed after 30 mins before scopolamine treatment and measured after 15 mins using acetylthiocholine iodide as subs | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1220556 | Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
| AID1722424 | Inhibition of electric eel AChE by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | New coumarin-benzotriazole based hybrid molecules as inhibitors of acetylcholinesterase and amyloid aggregation. |
| AID1076172 | Inhibition of human recombinant MAO-B using tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by fluorometric assay | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID725910 | Inhibition of BuChE in Sprague-Dawley rat serum by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors. |
| AID1353383 | Genotoxicity in human HepG2 cells assessed as induction of clastogenecity by measuring micronuclei index at 20 to 40 uM preincubated for 6 hrs followed by cytochalasin B addition measured after 28 hrs by Giemsa staining-based light microscopic method (Rvb | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1555985 | Inhibition of self-mediated amyloid beta (1 to 42) (unknown origin) aggregation at 100 uM incubated for 48 hrs by thioflavin-T fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1764089 | Inhibition of acetylcholinesterase (unknown origin) at 1 uM | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | The structural simplification of lysergic acid as a natural lead for synthesizing novel anti-Alzheimer agents. |
| AID1568792 | Reversible inhibition of equine serum BuChE assessed as enzyme activity at 0.1 times IC50 using butyrylthiocholine iodide as substrate measured at 120 mins by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1195140 | Effect on scopolamine-induced cognitive dysfunction in albino Swiss CD-1 mouse assessed as reduction in step-through latency time during retention trial at 5 to 10 mg/kg, ip administered 1 hr before the acquisition trial measured 24 hrs after acquisition | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with β-amyloid anti-aggregation properties and beneficial effects on memory in vivo. |
| AID361792 | Neuroprotective activity in rat PC12 cells assessed as inhibition of H2O2-induced neurotoxicity at 0.1 uM after 2 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | 2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity. |
| AID1738337 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer's disease. |
| AID1556434 | Metabolic stability in rat liver microsomes assessed as intrinsic clearance incubated for 20 to 60 mins in presence of metabolic phase 1 cofactors by HPLC-LC/MS analysis | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | 2-Aminoimidazole-based antagonists of the 5-HT |
| AID1338123 | Inhibition of recombinant human HFIP-pretreated amyloid beta (1 to 42) self-induced aggregation at 10 uM measured every 300 sec up to 28 hrs by thioflavin T-based fluorometric assay relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation. |
| AID635871 | Inhibition of equine serum BuchE using butyrylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | 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 di |
| AID1309429 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Design, synthesis and evaluation of novel indandione derivatives as multifunctional agents with cholinesterase inhibition, anti-β-amyloid aggregation, antioxidant and neuroprotection properties against Alzheimer's disease. |
| AID1055209 | Activity at rat liver TrxR at 15 uM measured for 10 mins in presence of NADPH relative to control | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID1453103 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease. |
| AID1195742 | Inhibition of recombinant human AChE expressed in HEK293 cells preincubated for 15 mins | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | 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. |
| AID1311919 | Inhibition of human erythrocyte ACHE preincubated for 6 mins followed by addition of acetylcholine iodide as substrate by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1635509 | Neuroprotective activity in Wistar rat brain hippocampus assessed as attenuation of Abeta (1 to 42) insult-induced increase in Abeta (1 to 42) expression level at 5 mg/kg, po administered for 15 days by Western blot analysis | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1655645 | Inhibition of human BChE using butyrylthiocholineiodide as substrate measured for every 30 sec for 5 mins by Ellman's method | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor. |
| AID1367022 | Antialzheimer activity in Swiss albino mouse brain assessed as reversal of scopolamine-induced reduction of TBARS level at 2 mg/kg, ip (Rvb = 26.51 +/- 0.79 nM/mg) | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Exploration of multi-target potential of chromen-4-one based compounds in Alzheimer's disease: Design, synthesis and biological evaluations. |
| AID771355 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 2 mins by Ellman's method | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Design, synthesis, biological evaluation and docking study of 5-oxo-4,5-dihydropyrano[3,2-c]chromene derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID1055219 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID1702417 | Inhibition of rat serum BChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1596488 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | A multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer's disease. |
| AID241560 | Inhibitory concentration against human plasma Butyrylcholinesterase | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine. |
| AID1225704 | Inhibition of Cu2+-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM after 24 hrs by thioflavin-T based fluorescence assay | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID49085 | Change in response to vagal stimulation was detected in anaesthetised cats on administration of the compound | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. |
| AID1612694 | Cognition enhancing effect in ICR mouse model of scopolamine-induced memory impairment assessed as spontaneous alteration at 5 mg/kg by Y-maze test (Rvb = 45.14%) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone. |
| AID311932 | Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID1556435 | Metabolic stability in rat liver microsomes assessed as half life incubated for 20 to 60 mins in presence of metabolic phase 1 cofactors by HPLC-LC/MS analysis | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | 2-Aminoimidazole-based antagonists of the 5-HT |
| AID1736859 | Inhibition of human erythrocyte AChE using acetylthiocholine as substrate measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | 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. |
| AID1557176 | Selectivity index, ratio of IC50 for equine serum BuChE using S-butyrylthiocholine chloride as substrate to IC50 for electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19 | The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1569982 | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1736869 | Cytotoxicity against HFF cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | 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. |
| AID1076771 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 100 nM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 2 | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1201374 | In vitro blood-brain barrier permeability at pH 7.4 by UV detection and HPLC based PAMPA method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Blood-brain barrier permeable anticholinesterase aurones: synthesis, structure-activity relationship, and drug-like properties. |
| AID1261741 | Cognitive enhancing effect in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as swimming path length in virtual platform at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by Morris water ma | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1225707 | Inhibition of human AChE-induced amyloid beta (1 to 40) (unknown origin) aggregation at 100 uM by thioflavin-T based fluorescence assay | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID44294 | Inhibitory concentration against Butyrylcholinesterase (BuChE) from human serum | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | Aminopyridazines as acetylcholinesterase inhibitors. |
| AID1552602 | In vivo antioxidant activity in albino mouse assessed as decrease in scopolamine-induced MDA level in brain at 5 mg/kg, po administered once daily for 7 days followed by scopolamine challenge by TBARS assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1703015 | Inhibition of recombinant electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by addition of substrate and measured after 20 mins by DTNB reagent based Ellman's method | 2020 | European journal of medicinal chemistry, Sep-01, Volume: 201 | The structure-based optimization of δ-sultone-fused pyrazoles as selective BuChE inhibitors. |
| AID1552617 | Reversal of scopolamine-induced amnesic effect in albino mouse assessed as increase in transfer latency time of acquisition trial at 5 mg/kg, po administered once daily for 7 days followed by scopolamine challenge and subsequent training session for 5 min | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1292351 | Selectivity ratio of IC50 for horse serum BChE to IC50 for electric eel AChE | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Biological evaluation of synthetic α,β-unsaturated carbonyl based cyclohexanone derivatives as neuroprotective novel inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID388546 | Inhibition of acetylcholinesterase in Wistar rat brain homogenate by Ellman's method | 2008 | Bioorganic & medicinal chemistry, Dec-01, Volume: 16, Issue:23 | Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity. |
| AID1311209 | Effective permeability of the compound at 100 uM at pH 7.4 after 3 to 6 hrs by PAMPA | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Design, synthesis and in vitro evaluation of benzothiazole-based ureas as potential ABAD/17β-HSD10 modulators for Alzheimer's disease treatment. |
| AID1217706 | Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1317859 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-aggregation at 25 uM measured after 48 hrs by ThT-assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID44133 | Inhibition of Equine Butyrylcholinesterase | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1 | Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors. |
| AID1773286 | Anti-alzheimer activity against oligomerized-amyloid beta (1 to 42) peptide-induced cognitive dysfunction ICR mouse model assessed as simplification of trajectories to the platform at 15 mg/kg, po administered from day 3 to 14 by Morris water maze test | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID1635496 | Neuroprotective effect in Swiss albino mouse assessed as increase in scopolamine-induced platform area crossings at 5 mg/kg, po 30 mins prior to scopolamine challenge administered for 9 days measured for last 5 days of treatment by Morris water maze test | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1421882 | Inhibition of human AChE using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors. |
| AID31777 | Tested for inhibition of AChE-induced Abeta aggregation in the peripheral sites of the human enzyme at a concentration of 100 uM | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | 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. |
| AID1545337 | Inhibition of rat serum butyrylcholinesterase using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID1317862 | Antioxidant activity assessed as AAPH radical scavenging activity measured as trolox equivalents preincubated for 15 mins followed by AAPH challenge measured every min for 80 mins by ORAC-FL assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID1635510 | Neuroprotective activity in Wistar rat brain hippocampus assessed as attenuation of Abeta (1 to 42) insult-induced increase in p-Tau expression level at 5 mg/kg, po administered for 15 days by Western blot analysis | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1854697 | Inhibition of equine serum BuChE using butyrylthiocholine as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric based Ellman's method | 2022 | Bioorganic & medicinal chemistry, 10-01, Volume: 71 | Synthesis and biological evaluation of 4-hydroxy-methylpiperidinyl-N-benzyl-acylarylhydrazone hybrids designed as novel multifunctional drug candidates for Alzheimer's disease. |
| AID724166 | Inhibition of bovine acetylcholinesterase using acetylcholine iodide as substrate incubated for 20 mins prior to substrate addition measured after 3 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase. |
| AID1445561 | Toxicity in ip dosed CD1 mouse assessed as mortality administered as qd after 48 hrs | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a "Bio-Oxidizable" Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation. |
| AID1569987 | Antioxidant activity assessed as AAPH radical scavenging activity preincubated for 15 mins followed by AAPH addition measured every min for 90 mins by ORAC-FL assay relative to trolox | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1633173 | Inhibition of amyloid beta 1 to 42 (unknown origin) self aggregation up to 20 uM after 48 hrs by thioflavin T-based fluorometric assay relative to donepezil | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1383685 | Inhibition of electric eel AChE-induced amyloid beta (1 to 42) aggregation after 48 hrs by thioflavin T fluorescence spectroscopic method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
| AID1906407 | Inhibition of AChE in glyceraldehyde-exposed human SH-SY5Y differentiated neuronal cells using acetylthiocholine as substrate by Ellman's spectrophotometric method | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1517853 | Selectivity index, ratio of IC50 for human BuChE to IC50 for human AChE | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1489005 | Inhibition of AChE (unknown origin) using acetylthiocholine as substrate by Ellman's method | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 | Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease. |
| AID1701448 | Anti-VaD activity against UCCAO-induced spatial memory deficient C57BL/6J mouse model assessed as improvement in spatial learning and memory by measuring increased the frequency of platform site crossing at 1 mg/kg, po administered for 21 days by Morris w | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Rational Design of 2-Chloroadenine Derivatives as Highly Selective Phosphodiesterase 8A Inhibitors. |
| AID594989 | Inhibition of human recombinant AChE after 20 mins using acetylthiocholine iodide as a substrate by Ellman's assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | 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. |
| AID1668321 | Inhibition of LPS-induced IL6 production in human BV2 cells at 20 ug/ml preincubated for 4 hrs followed by LPS stimulation and measured after 24 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12 | Betulin isolated from Pyrola incarnata Fisch. inhibited lipopolysaccharide (LPS)-induced neuroinflammation with the guidance of computer-aided drug design. |
| AID1330763 | Inhibition of copper-mediated aggregation of amyloid beta (1 to 42 residues) (unknown origin) at 40 uM incubated for 46 to 48 hrs by thioflavin-T binding assay relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1673644 | Inhibition of human erythrocytes AChE-induced amyloid beta (1 to 42) aggregation assessed as normalized fluorescence intensity at 5 to 20 uM after 48 hrs by thioflavin T-based fluorometric assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1738102 | Inhibition of recombinant human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by spectrophotometry based Ellman's method | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1752600 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease. |
| AID1325657 | Inhibition of electric eel AChE preincubated for 15 mins followed by acetylthiocholine iodide substrate addition measured for 5 mins by Ellman's spectrophotometric method | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Design, synthesis, and AChE inhibitory activity of new benzothiazole-piperazines. |
| AID1407159 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID1736969 | Inhibition of human BChE assessed as residual activity at IC50 concentration relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID454343 | Inhibition of BChE in rat serum after 15 mins by modified Ellman's method | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors. |
| AID1456002 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured at 12 secs interval for 5 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
| AID1597705 | Inhibition of human BChE using butyrylthiocholine as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | 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. |
| AID1335935 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-6 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1353746 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one scaffold derivatives: Synthesis and biological evaluation as selective BuChE inhibitors. |
| AID1556452 | Reversal of scopolamine induced cognitive impairment impairment in Sprague-Dawley rat at 1 mg/kg, po pre treated for 2 hrs followed by scopolamine addition further treated for 30 mins and measured after 1 hr by novel object recognition test | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | 2-Aminoimidazole-based antagonists of the 5-HT |
| AID1530607 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Investigating alkyl nitrates as nitric oxide releasing precursors of multitarget acetylcholinesterase-monoamine oxidase B inhibitors. |
| AID1335937 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-8 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1473874 | Drug concentration at steady state in human at 5 to 10 mg, po after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1709284 | Memory improvement effect in Kunming mouse model of scopolamine-induced memory impairment assessed as increase in latency time at 5 mg/kg, ig administered once daily for 7 days followed by scopolamine challenge 30 mins prior to training on day 6 measured | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1501677 | Induction of neuronal differentiation in human SH-SY5Y cells assessed as neurite bearing cells at 0.0057 uM followed by culture medium replacement for every three days for 10 days by inverted-phase microscopic analysis relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID763836 | Activity at AChE in Charles Foster rat hippocampus assessed as substrate hydrolyzed per mg of protein at 5 mg/kg, po for 8 days by Ellman's method (Rvb = 47.50 +/- 0.84 mol/min) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1882049 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID1421297 | Displacement of [3H]DTG from S1R in P2 fraction of Hartley guinea pig whole brain after 90 mins by liquid scintillation counting method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID1752614 | Reversal of scopolamine induced cognitive memory impairment in C57BL/6 mouse assessed as escape latency time at 0.5 mg/kg, ip administered 30 mins prior to scopolamine injection daily for 14 days by Morris water maze test (Rvb = 33.58 +/-3.54 secs) | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease. |
| AID1906373 | Neuroprotective activity in human SH-SY5Y differentiated neuronal cells assessed as inhibition of GA-induced axon morphology defects at 0.5 uM by laser confocal microscope | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1338166 | Inhibition of AChE (unknown origin) at 1 uM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease. |
| AID1273118 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors. |
| AID1359870 | Inhibition of amyloid beta (1 to 42) (unknown origin)-induced cell death in human SH-SY5Y cells assessed as cell viability at 100 uM preincubated for 3 hrs followed by amyloid beta (1 to 42) addition measured after 24 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds. |
| AID1156022 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by spectrophotometer analysis | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and anti-cholinesterase activity of new 7-hydroxycoumarin derivatives. |
| AID1625115 | Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities. |
| AID1156023 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate by spectrophotometer analysis | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and anti-cholinesterase activity of new 7-hydroxycoumarin derivatives. |
| AID1320872 | Inhibition of human serum BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured for 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | 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. |
| AID1906376 | Neuroprotective activity in human SH-SY5Y differentiated neuronal cells assessed as inhibition of GA-induced cell death by measuring increase in cell viability at 0.5 to 5 uM measured after 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1888252 | Permeability of the compound in PBS/EtOH buffer (7:3) incubated for 16 hrs by PAMPA-BBB assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/α-synuclein aggregation inhibitors with neuroprotective effects. |
| AID1631830 | Inhibition of electric eel AChE using ACTI as substrate preincubated for 29 mins followed by substrate addition measured at 1 min intervals for 10 mins by Ellman's assay | 2016 | Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16 | Discovery and Structure-Activity Relationships of a Highly Selective Butyrylcholinesterase Inhibitor by Structure-Based Virtual Screening. |
| AID1480843 | Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity at 5 uM pretreated for 15 mins followed by APPH challenge measured every minute for 240 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1666045 | Improvement in cognition in ICR mouse model of Abeta(1-42)-induced cognition-impairment assessed as spontaneous alternation performance level at 15 mg/kg, po dosed from days 3 to 14 and measured on day 15 by Y maze test (Rvb = 34.43%) | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor. |
| AID1421290 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 50 uM after 48 hrs by MTS assay relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID404844 | Inhibition of human serum BChE by Ellman's assay | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1319304 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 100 uM measured after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18 | Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. |
| AID1633210 | Selectivity index, ratio of CC50 for human SH-SY5Y cells to IC50 for inhibition of mouse brain AChE | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID748746 | Antiamnesic activity in Charles Foster albino rat assessed as reduction in scopolamine-induced increase in transfer latency at 10 mg/kg, po administered for 8 days measured 30 mins post last dose by elevated plus maze task (Rvb = 62.50 +/- 0.76 s) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Design, synthesis and evaluation of some new 4-aminopyridine derivatives in learning and memory. |
| AID496882 | Inhibition of AChE-induced amyloid beta (1-40) aggregation | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy. |
| AID1520012 | Intrinsic clearance in rat liver microsomes up to 60 mins by HPLC-LC/MS analysis relative to control | |||
| AID1701392 | Inhibition of electric eel AChE at 1 uM using acetylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured for 10 mins by Ellman's method relative to control | 2021 | Bioorganic & medicinal chemistry, 01-01, Volume: 29 | Design, synthesis, and biological activity of novel semicarbazones as potent Ryanodine receptor1 inhibitors of Alzheimer's disease. |
| AID1657146 | Antialzheimer activity in scopolamine-induced Kunming mouse model of memory impairment assessed as increase in latency time at 5 mg/kg/day, ig for 7 days followed by training trial at 1 hr post dose on day 6 and subsequent scopolamine challenge at 30 mins | 2020 | Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8 | Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. |
| AID1335237 | Inhibition of electric eel AChE preincubated for 5 mins followed by acetylthiocholine iodide substrate addition measured after 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT |
| AID1736965 | Reversible inhibition of human AChE assessed as residual activity at 0.1 times of IC50 concentration relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1906372 | Neuroprotective activity in human SH-SY5Y differentiated neuronal cells assessed as inhibition of GA-induced neurite shortening by measuring increase in axon length at 0.5 uM by laser confocal microscope | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID44295 | Inhibitory potency was evaluated against isolated Butyrylcholinesterase | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | 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. |
| AID361791 | Selectivity ratio of IC50 for BuchE in rat serum to IC50 for AchE in rat cortex | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | 2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity. |
| AID1378882 | Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1068375 | Inhibition of horse serum BuChE using butyrylthiocholine as substrate by Ellman's method | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease. |
| AID1820947 | Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1739254 | Inhibition of BuChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase. |
| AID1906368 | Cytotoxicity against human SH-SY5Y cells assessed as maximum non-cytotoxic concentration by CellTiter-Glo luminescent assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1465302 | Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID323564 | Inhibition of AChE | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 | Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling. |
| AID1756758 | Cognitive enhancing effect in mouse model of scopolamine-induced memory impairment assessed as reduction in escape latency time at 8 to 12 mg/kg, IG QD for 3 days by channel water maze test | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID1416365 | Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 to 3 mins time interval by Ellman's method | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1252808 | Selectivity ratio of IC50 for human serum BuChE to IC50 for human recombinant AChE | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | New multifunctional melatonin-derived benzylpyridinium bromides with potent cholinergic, antioxidant, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1773287 | Anti-alzheimer activity against oligomerized-amyloid beta (1 to 42) peptide-induced cognitive dysfunction ICR mouse model assessed as improvement in alteration performance at 15 mg/kg, po administered from day 3 to 14 by Morris water maze test | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID238704 | Dissociation constant for inhibition of equine Butyrylcholinesterase (BuChE) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. |
| AID1379019 | Antioxidant activity assessed as inhibition of AAPH-induced peroxyl radical generation measured as trolox equivalent preincubated for 15 mins followed by AAPH addition measured every min for 120 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1465299 | Inhibition of equine serum BuChE incubated for 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1261782 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as pyknotic nucleus in dentate gyrus region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by he | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID670563 | Inhibition of human AChE using acetylthiocholine iodide as substrate after 5 mins by DTNB method | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14 | Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template. |
| AID30868 | In vitro inhibition of electric eel acetylcholinesterase | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID1578226 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Search for new multi-target compounds against Alzheimer's disease among histamine H |
| AID1374193 | Inhibition of self-induced aggregation of amyloid beta (1 to 42) (unknown origin) at 25 uM after 24 hrs by thioflavin T fluorescence method relative to control | 2018 | Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5 | Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment. |
| AID1261774 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as reduction of dead neurons in dentate gyrus region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last d | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1261737 | Cognitive enhancing effect in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as virtual platform crossing at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by Morris water maze assay (Rvb = | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1311915 | Inhibition of equine BCHE preincubated for 6 mins followed by addition of S-butyrylcholine iodide as substrate by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1480940 | Neuroprotective activity against oxygen glucose deprivation/re-oxygenation-induced mitochondrial oxidative stress in human SH-SY5Y cells assessed as cell survival at 0.3 uM pretreated for 24 hrs followed by 4 hrs incubation under oxygen glucose deprivatio | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | 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. |
| AID1596487 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Aug-01, Volume: 175 | A multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer's disease. |
| AID1568788 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1815194 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID1199518 | Inhibition of Electrophorus electricus AChE after 5 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID763842 | Cognitive enhancing effect in Charles Foster rat assessed as reversal of scopolamine-induced amnesia measured as transfer latency at 5 mg/kg, po for 8 days administered 1 hr prior to scopolamine-challenge on day 7 measured on same day by elevated plus maz | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1771841 | Inhibition of equine serum BuChE using BTC as substrate at 10 uM preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT |
| AID1707551 | Drug concentration in wild type C57BL6 mouse plasma at 2 mg/kg, ip thrice a week for 2 weeks observed after 4 hrs post last dose by HPLC/MS/MS analysis | |||
| AID1317861 | Inhibition of electric eel AChE-mediated amyloid beta (1 to 42) (unknown origin) co-aggregation at 100 uM measured after 48 hrs by ThT-assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID1820951 | Reversible inhibition of equine serum BChE assessed as residual enzyme activity using butyrylthiocholine iodide as substrate at 0.1 times IC50 incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1501301 | Binding affinity to 59Fe2+ in human SK-N-MC cells labeled with 59Fe2-transferrin assessed as Fe release at 25 uM after 3 hrs by gamma scintillation counting method relative to total cellular 59Fe2+ (Rvb = 6%) | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1537659 | Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate by Ellman's method | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1292350 | Inhibition of horse serum BChE using butrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 10 mins by modified Ellman's method | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Biological evaluation of synthetic α,β-unsaturated carbonyl based cyclohexanone derivatives as neuroprotective novel inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID1465276 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | 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. |
| AID763841 | Cognitive enhancing effect in Charles Foster rat assessed as reversal of scopolamine-induced amnesia measured as transfer latency at 10 mg/kg, po for 8 days administered 1 hr prior to scopolamine-challenge on day 7 measured on same day by elevated plus ma | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID745544 | Inhibition of acetylcholine esterase (unknown origin) using acetylthiocholine as substrate incubated for 15 mins prior to substrate addition measured after 5 mins by spectrophotometry | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Triazolothiadiazoles and triazolothiadiazines--biologically attractive scaffolds. |
| AID1585835 | Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID282011 | Inhibition of AChE mediated aggregation of amyloid beta relative to control | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties. |
| AID1465286 | Selectivity index, ratio of IC50 for human serum BChE to IC50 for human erythrocyte AChE | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | 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. |
| AID1596160 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured every minute for 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Jul-15, Volume: 174 | Benzoic acid-derived nitrones: A new class of potential acetylcholinesterase inhibitors and neuroprotective agents. |
| AID1810374 | Inhibition of mouse AChE using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method | |||
| AID1707761 | Reversible inhibition of recombinant human AChE expressed in HEK293 cells assessed as residual activity at 0.1 times IC50 using acetylthiocholine iodide as substrate preincubated for 30 mins followed by 100-fold dilution in presence of substrate and measu | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1695766 | Effective permeability of compound in PBS buffer at pH 7.4 at 25 ug/ml incubated for 20 hrs by PAMPA-BBB assay | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions. |
| AID1633668 | Permeability of the compound at pH 7.4 PBS buffer at 100 uM measured upto 6 hrs by PAMPA-BBB assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
| AID1695757 | Antioxidant activity assessed as DPPH radical scavenging activity at 20 uM after 30 mins under dark condition by DPPH assay relative to control | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions. |
| AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1353748 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one scaffold derivatives: Synthesis and biological evaluation as selective BuChE inhibitors. |
| AID1070081 | GPx-like activity of the compound assessed as GSH-mediated H2O2 reduction at 80 uM at pH 7.5 measured for 10 secs by spectrophotometric analysis (Rvb = 39.46 +/- 1.5 uM/min) | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease. |
| AID1427878 | Elimination half life in human | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Targeting Alzheimer's disease by investigating previously unexplored chemical space surrounding the cholinesterase inhibitor donepezil. |
| AID1824586 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as half life measured upto 45 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID31621 | Inhibitory potency was evaluated against recombinant human AChE | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | 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. |
| AID1635486 | Inhibition of human erythrocyte AChE-induced Abeta (1 to 42) aggregation at 10 uM incubated for 24 hrs by thioflavin-T fluorescence assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1709285 | Memory improvement effect in Kunming mouse model of scopolamine-induced memory impairment assessed as reduction in number of errors at 5 mg/kg, ig administered once daily for 7 days followed by scopolamine challenge 30 mins prior to training on day 6 meas | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1711762 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Development of cyanopyridine-triazine hybrids as lead multitarget anti-Alzheimer agents. |
| AID31502 | Inhibitory potency was evaluated against recombinant human AChE | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | 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. |
| AID1633207 | Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1195743 | Inhibition of recombinant human BuChE expressed in HEK293 cells preincubated for 15 mins | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | 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. |
| AID1077082 | Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM after 24 hrs by thioflavin T fluorescence method | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1156823 | Inhibition of BuChE (unknown origin) after 5 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | 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. |
| AID1195131 | Inhibition of horse serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins by Ellman method | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with β-amyloid anti-aggregation properties and beneficial effects on memory in vivo. |
| AID1156822 | Inhibition of AChE (unknown origin) after 5 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | 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. |
| AID31964 | In vitro inhibitory effect on rat Acetylcholinesterase | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15 | Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation. |
| AID1367023 | Antialzheimer activity in Swiss albino mouse brain assessed as reversal of scopolamine-induced reduction of AChE activity assessed per mg protein at 2 mg/kg, ip (Rvb = 1.25 +/- 0.04 nM/min/mg) by spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Exploration of multi-target potential of chromen-4-one based compounds in Alzheimer's disease: Design, synthesis and biological evaluations. |
| AID1421289 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 25 uM after 48 hrs by MTS assay relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID1738132 | Ex vivo inhibition of BChE in brain of scopolamine-induced Swiss albino mouse model of amnesia at 5 mg/kg, po administered for 7 days and observed after 30 mins before scopolamine treatment and measured after 15 mins using butyryl thiocholine iodide as su | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1762425 | Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters. |
| AID1055210 | Antioxidant activity assessed as peroxynitrite scavenging activity by Evans blue dye-based spectrophotometric analysis relative to control | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID1820990 | Anti-alzheimer activity against scopolamine-induced cognitive dysfunction mouse model assessed as change in neuron damage in hippocampal CA1 region at 5 mg/kg, po measured after 10 days by Nissl staining based assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID47966 | Effective dose required for the reversal of vecuronium-induced neuromuscular block in-vivo in Chloaralose anaesthetised cats | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. |
| AID323565 | Inhibition of histamine H3 receptor | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 | Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling. |
| AID1421282 | Antioxidant activity assessed as DPPH free radical scavenging at 465 uM after 20 mins by UV-Vis spectrophotometric analysis relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID1693580 | Neuroprotective activity against OA-induced cytotoxicity in human SH-SY5Y cells assessed as increase in cell viability incubated for 1 hr followed by OA stimulation and measured after 24 hrs by CCK8 assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID722584 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate after 60 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Additional acetyl cholinesterase inhibitory property of diaryl pyrazoline derivatives. |
| AID1631831 | Selectivity ratio of IC50 for human plasma BuChE to IC50 for human erythrocyte AChE | 2016 | Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16 | Discovery and Structure-Activity Relationships of a Highly Selective Butyrylcholinesterase Inhibitor by Structure-Based Virtual Screening. |
| AID1557174 | Inhibition of human recombinant MAO-B using kynuramine as substrate measured after 30 mins by fluorimetric assay | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19 | The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1191629 | Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Synthesis, biological evaluation and molecular docking study of novel piperidine and piperazine derivatives as multi-targeted agents to treat Alzheimer's disease. |
| AID1368601 | Inhibition of AchE in brain homogenates of scopolamine-induced albino mouse memory deficit model at 1 uM using acetylthiocholine iodide as substrate incubated for 10 mins measured for 2 mins by Ellman's method relative to control | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1570003 | Antialzheimer activity in scopolamine-induced memory impairment Kunming mouse model assessed as latency time at 5 mg/kg, po treated with compound 1 hr before training trial followed by 30 mins later administration with scopolamine and measured 24 hrs afte | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1555997 | Neuroprotective activity against H2O2 induced cytotoxicity in rat PC12 cells assessed as cell viability at 10 uM pretreated for 3 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay (Rvb = 35.69 to 50.26%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1533629 | In vivo antioxidant activity in Swiss albino mouse brain assessed as increase in GSH level at 1 mg/kg, ip qd pretreated for 1 hr followed by scopolamine addition | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1555999 | Neuroprotective activity against H2O2 induced cytotoxicity in rat PC12 cells assessed as cell viability at 50 uM pretreated for 3 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay (Rvb = 35.69 to 50.26%) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1330752 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1367015 | Inhibition of rat brain AChE using acetylthiocholine iodide as substrate by spectroscopic method | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Exploration of multi-target potential of chromen-4-one based compounds in Alzheimer's disease: Design, synthesis and biological evaluations. |
| AID1889349 | Reversible inhibition of human AChE assessed as restoration of enzyme activity at 0.1 time of IC50 concentration incubated for 60 mins by dilution method relative to control | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1820948 | Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1625110 | Inhibition of HFIP-pretreated human amyloid beta (1 to 42) self-induced aggregation at 25 uM measured after 24 hrs by thioflavin-T fluorescence assay relative to control | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities. |
| AID1199524 | Inhibition of human recombinant amyloid beta (1 to 42) self-induced aggregation at 10 uM after 24 hrs by thioflavin-T based fluorometric assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID1322905 | Selectivity index, ratio of IC50 for human recombinant MAOB to IC50 for human recombinant MAOA | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation. |
| AID1593218 | Inhibition of human AChE-induced amyloid beta aggregation (1-40) (unknown origin) aggregation at 100 uM incubated for 24 hrs by thioflavin T based fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease. |
| AID1738104 | Inhibition of recombinant equine serum BuChE at 20 uM using butyryl thiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by spectrophotometry based Ellman's method relative to control | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1076770 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 1 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 24 | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1756693 | Selectivity index, ratio of IC50 for rat serum BuChE using S-butyrylthiocholine iodide as substrate to IC50 for rat cortex homogenate acetylcholinesterase using acetylthiocholine iodide as substrate | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
| AID763830 | Cognitive enhancing effect in Wistar rat assessed as reversal of learning impairment measured as transfer latency at 5 mg/kg, po for 8 days measured on second day of test by elevated plus maze test (Rvb = 66.824 +/- 0.47 seconds) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1217712 | Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1691666 | Inhibition of human serum BuChE assessed as residual activity at 0.1 times IC50 using acetylcholine iodide as substrate measured after dilution by Ellman's method relative to control | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1773285 | Anti-alzheimer activity against scopolamine-induced cognitive dysfunction mouse model assessed as increase in swimming time in the target quadrant crossing at 10 mg/kg, ip measured after 60 mins by Morris water maze test | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID404842 | Inhibition of bovine erythrocyte AChE by Ellman's assay | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1506097 | Cognitive enhancing effect in amyloid beta (1 to 42)-induced dementia Balb/c mouse model assessed as protection against spatial memory impairment by measuring latency to find food on third and fourth days of test at 10 mg/kg, po qd via gavage for 17 days | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15 | Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile. |
| AID1633202 | Inhibition of mouse brain AChE using acetylthiocholine iodide as substrate measured after 30 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1199521 | Inhibition of human recombinant AChE after 5 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID282830 | Inhibition of human AChE-induced beta amyloid peptide(1-40) aggregation by thioflavin T-based fluorometric assay | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease. |
| AID73711 | In vitro reversal of vecuronium-induced neuromuscular block in guinea pig hemi-diaphragm. | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. |
| AID1772662 | Cognitive enhancing effect in mouse model of scopolamine-induced amnesia assessed as decrease in escape latency at 10 mg/kg/day, po measured by Morris water maze test | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID658003 | Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 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. |
| AID1609227 | Improvement in learning and spatial memory in icv infused amyloid beta (1 to 42)-induced Wistar rat model of Alzheimer's disease assessed as reduction in degeneration of neuron in hippocampal region at 5 mg/kg, po administered daily for 7 days starting fr | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1374194 | Inhibition of cupric ion-mediated amyloid beta (1 to 42) aggregation at 25 uM after 24 hrs by thioflavin T fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5 | Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment. |
| AID1473873 | AUC in human at 5 to 10 mg, po after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID768523 | Selectivity index, ratio of IC50 for human plasma BuChE to IC50 for purified human erythrocyte AChE | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis, pharmacological assessment, and molecular modeling of 6-chloro-pyridonepezils: new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease. |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1456005 | Non-competitive inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured at 12 secs interval for 5 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer's disease. |
| AID1906409 | Antioxidant activity against okadaic acid-induced ROS generation in human SH-SY5Y cells assessed as reduction in DCF fluorescence intensity at 0.5 uM pretreated for 24 hrs followed by okadaic acid addition for 24 hrs by DCFH-DA dye based fluorescence anal | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1421286 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 25 uM after 24 hrs by MTS assay relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID1338115 | Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation. |
| AID1773259 | Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM incubated for 2 hrs by microplate reader method | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease. |
| AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1076765 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 10 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rela | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1673636 | Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1591467 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman method | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Naphthalene-triazolopyrimidine hybrid compounds as potential multifunctional anti-Alzheimer's agents. |
| AID1738336 | Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer's disease. |
| AID1261757 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as irregular shape in CA1 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxylin a | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1888431 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 5 mins by DTNB-reagent based Ellman's method | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1152907 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 5 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1585837 | Antioxidant activity assessed as trolox equivalent of APPH-induced radical scavenging activity at 5 uM preincubated for 15 mins followed by AAPH addition measured every minute for 90 mins by ORAC fluorescein assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1225694 | Inhibition of AChE in human erythrocytes using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1698418 | Displacement of propidium iodide from PAS region of human AChE at 10 uM incubated for 6 hrs by fluorescence assay relative to control | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1407155 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID1430428 | Inhibition of equine serum BCHE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 5 mins by spectrophotometry based Ellman method | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | 3,4-Dihydroquinazoline derivatives inhibit the activities of cholinesterase enzymes. |
| AID1070084 | Inhibition of electric eel acetylcholinesterase using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease. |
| AID1193152 | Inhibition of Electrophorus electricus AChE pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents. |
| AID1465275 | Inhibition of equine serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | 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. |
| AID1767554 | Inhibition of human amyloid beta (25 to 35) self-induced aggregation at 100 uM after 48 hrs by thioflavin-T fluorescence relative to control | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant. |
| AID1176163 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1635513 | Neuroprotective activity in Swiss albino mouse brain assessed as inhibition of scopolamine-induced elevation in AChE level at 5 mg/kg, po administered 30 mins prior to scopolamine challenge administered for 9 days by Ellman assay relative to vehicle-treat | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1076176 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 5 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1498851 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 2 mins followed by substrate addition and measured after 2 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Design, synthesis and evaluation of novel bivalent β-carboline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID48700 | Mean arterial pressure change was detected in anaesthetised cats on administration of the compound | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. |
| AID1436082 | Inhibition of BuChE in rat serum using butyrylthiocholine as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease. |
| AID1884593 | In vivo inhibition of AChE in hippocampus of aggregated Abeta(25-35)-induced Alzheimer's disease C57BL/6 mouse model at 2 mg/kg, iv measured after 2 hrs by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID1846074 | Inhibition of equine BuChE by Ellman's method | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | A review on ferulic acid and analogs based scaffolds for the management of Alzheimer's disease. |
| AID1889345 | Reversible inhibition of human AChE assessed as enzyme recovery activity at IC50 concentration by dilution method relative to control | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1201382 | Retention time of the compound by HPLC-fluorescence method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Blood-brain barrier permeable anticholinesterase aurones: synthesis, structure-activity relationship, and drug-like properties. |
| AID1609207 | Displacement of propidium iodide from PAS region of electric eel AChE at 50 uM incubated for 6 hrs by fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1702494 | Antialzheimer activity against 3 dpf zebrafish model of AlCl3-induced AD assessed as efficacy on motility distance at 8 uM relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1533616 | Cognitive enhancing effect in Swiss albino mouse assessed as reversal of scopolamine-induced reduction in spontaneous alteration score at 1 mg/kg, ip qd pretreated for 1 hr followed by scopolamine addition by Y-maze test | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1723545 | Protection against amyloid beta oligomer-induced cytotoxicity in human SH-SY5Y cells expressing miRNA-15b assessed as cell viability at 10 uM after 72 hrs by MTT assay relative to control | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | MicroRNA-Based Multitarget Approach for Alzheimer's Disease: Discovery of the First-In-Class Dual Inhibitor of Acetylcholinesterase and MicroRNA-15b Biogenesis. |
| AID1609216 | Ex vivo inhibition of AChE in brain of scopolamine-induced Wistar rat model of amnesia at 5 mg/kg pretreated for 7 days followed by scopolamine challenge and measured after 30 mins using acetylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID677019 | Antiamnesic activity in mouse assessed as inhibition of scopolamine-induced escape latency time at 25 mg/kg, ip measured on day 1 by Morris water maze test (Rvb = 89.7 +/- 3.8 secs) | 2012 | Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1 | Synthesis and evaluation of novel 4-[(3H,3aH,6aH)-3-phenyl)-4,6-dioxo-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazol-5(3H,6H,6aH)-yl]benzoic acid derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents. |
| AID657793 | Selectivity ratio of IC50 for mitochondrial MAO-B in rat liver homogenates to IC50 for mitochondrial MAO-A in rat liver homogenates | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 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. |
| AID1569977 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease. |
| AID1427509 | Inhibition of rat serum BuChE using S-butylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
| AID1498422 | Inhibition of horse serum BChE using butyrylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured after 20 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis, structure-activity relationship and molecular docking studies of 3-O-flavonol glycosides as cholinesterase inhibitors. |
| AID1693640 | Cognitive enhancing effect in ICR mouse model of scopolamine-induced cognitive dysfunction assessed as shorter distances travelled before reaching the escape platform at 15 mg/kg, po by Morris water maze test | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID1320874 | Inhibition of human recombinant MAOA using p-tyramine as substrate incubated for 15 mins by fluorimetric method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | 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. |
| AID1076173 | Inhibition of human recombinant MAO-A using tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by fluorometric assay | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1389178 | Inhibition of equine serum BChE at 10 uM using S-butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease. |
| AID781330 | pKa (acid-base dissociation constant) as determined by potentiometric titration | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID1351942 | Displacement of propidium iodide from electric eel AChE at 10'-5 M after 6 hrs by fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine "bio-oxidizable" prodrugs: Synthesis, biological evaluation and structure-activity relationship. |
| AID1635512 | Antiapoptotic activity in Wistar rat brain hippocampus assessed as attenuation of Abeta (1 to 42) insult-induced increase in cleaved PARP expression level at 5 mg/kg, po administered for 15 days by Western blot analysis | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1709287 | Reversal of scopolamine-induced memory impairment in Kunming mouse assessed as increase in ACh level in cerebral cortex at 5 mg/kg, ig administered once daily for 7 days followed by scopolamine challenge 30 mins prior to training trail on day 6 measured o | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1480942 | Permeability of the compound at pH 7.4 at 1 mg/ml after 4 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | 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. |
| AID1705722 | Inhibition of electric eel AChE at 10 uM using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every minute for 10 mins by DTNB-reagent based Ellman's method relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase. |
| AID1772660 | In vivo inhibition of AChE in ICR mouse intestine at 10 mg/kg, po measured after 1.5 hrs by Ellman method relative to control | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID1076764 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 100 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rel | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1057006 | Mixed-type inhibition of human recombinant AChE-induced beta-amyloid (1 to 40) aggregation at 100 uM after 48 hrs by thioflavin T fluorescence spectroscopic analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. |
| AID1609198 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured for 1 min by DTNB reagent-based spectrophotometric analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1407166 | Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID1257005 | Antioxidant activity assessed as DPPH scavenging activity at 10 to 60 ug/ml after 30 mins | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease. |
| AID1385851 | Reversal of scopolamine-induced cognitive impairment in rhesus monkey assessed increase in novel object retrieval at 0.3 mg/kg by novel object recognition test | 2018 | ACS medicinal chemistry letters, Aug-09, Volume: 9, Issue:8 | Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor. |
| AID1506100 | Cognitive enhancing effect in amyloid beta (1 to 42)-induced dementia Balb/c mouse model assessed as protection against spatial memory impairment by measuring reduction in total errors to find food on third and fourth days of test at 10 mg/kg, po qd via g | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15 | Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID361793 | Neuroprotective activity against rat PC12 cells assessed as inhibition of H2O2-induced neurotoxicity at 0.5 uM after 2 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | 2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity. |
| AID1407173 | Mixed-type inhibition of human AChE using acetylthiocholine chloride as substrate incubated for 5 mins followed by substrate addition by Lineweaver-Burk plot analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID1809144 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate incubated for 15 to 20 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, synthesis, and cholinesterase inhibition assay of liquiritigenin derivatives as anti-Alzheimer's activity. |
| AID1815192 | Selectivity index, ratio of IC50 for rat serum BChe to IC50 for rat cortex AChE | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1820945 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured after 15 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID635810 | Inhibition of AChE in rat cortex homogenates using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID1633180 | Reversal of scopolamine-induced spatial memory impairment in Wistar rat model of amnesia assessed as decrease in transfer latency at 5 mg/kg, po administered once daily for 1 week followed by scopolamine challenge 30 mins prior to test by elevated plus ma | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1353380 | Cytotoxicity against human SH-SY5Y cells assessed as inhibition of cell viability after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1657141 | Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells at 10 uM using kynuramine as substrate measured after 30 mins by fluorescence based assay relative to control | 2020 | Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8 | Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. |
| AID1762429 | Inhibition of human BuchE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters. |
| AID1290887 | Inhibition of rat serum butyrylcholinesterase using butyrylthiocholine iodide substrate after 15 mins by spectrophotometric method | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease. |
| AID482854 | Inhibition of equine serum BuChE by Ellman's method | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
| AID1374196 | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells at 10 uM using kynuramine as substrate after 30 mins by fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5 | Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment. |
| AID1390031 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
| AID1162591 | Selectivity index, ratio of IC50 for human recombinant BuChE to IC50 for human recombinant AChE | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | 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. |
| AID1279141 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1673635 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1416361 | Inhibition of recombinant human MAO-A assessed as reduction in H2O2 production using p-tyramine as substrate preincubated for 15 mins followed by substrate addition by Amplex red reagent based fluorescence assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1368599 | Cognition enhancing effect in albino mouse assessed as reversal of scopolamine-induced memory deficit by measuring latency time at 0.5 mg/kg, ip treated 5 mins post scopolamine challenge by step down passive avoidance test (Rvb = 68.16 +/- 0.4 sec) | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction. |
| AID1378353 | Inhibition of recombinant human BACE1 at 20 uM preincubated with enzyme followed by H-RE(EDANS)EVNLDAEFK(Dabcyl)R-OH as substrate measured after 60 mins by fluorimetric assay relative to control | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates. |
| AID1076772 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 10 nM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 24 | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1809147 | Cytotoxicity against human PBMC assessed as reduction in cell viability | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, synthesis, and cholinesterase inhibition assay of liquiritigenin derivatives as anti-Alzheimer's activity. |
| AID1900712 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID1379020 | Inhibition of HFIP pretreated amyloid beta (1 to 42) (unknown origin) self-aggregation at 20 uM after 48 hrs by thioflavin T fluorescence assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1701451 | Anti-VaD activity against UCCAO-induced spatial memory deficient C57BL/6J mouse model assessed as improvement in spatial learning and memory by measuring increase in latency time at 1 mg/kg, po administered for 21 days by passive avoidance test | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Rational Design of 2-Chloroadenine Derivatives as Highly Selective Phosphodiesterase 8A Inhibitors. |
| AID1532592 | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Novel multitarget-directed ligands targeting acetylcholinesterase and σ |
| AID1261779 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as pyknotic nucleus in CA1 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hematoxylin | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1421291 | Neuroprotection against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as reduction in ROS generation at 10 uM preincubated for 3 hrs followed by DCFDA addition for 45 mins and subsequent co-treatment with compound and H2O2 for 24 hrs by fl | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID1906369 | Inhibition of AChE in human SH-SY5Y differentiated neuronal cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser199 residue at 0.001 to 5 uM by ELISA | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1202691 | Inhibition of electric eel AChE pre-incubated for 3 mins before acetylthiocholine substrate addition by Lineweaver-Burk plot | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Design, synthesis and anticholinesterase activity of novel benzylidenechroman-4-ones bearing cyclic amine side chain. |
| AID1633205 | Inhibition of mouse brain AChE at 10 uM using acetylthiocholine iodide as substrate measured after 30 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1126181 | Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 10 mins before substrate addition after 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis, cytotoxicity and molecular modelling studies of new phenylcinnamide derivatives as potent inhibitors of cholinesterases. |
| AID1322907 | Selectivity ratio of IC50 for human recombinant AChE to IC50 for human recombinant BuChE | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation. |
| AID707699 | Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1407169 | Selectivity index, ratio of IC50 for human serum BuChE to IC50 for human erythrocyte AChE | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties. |
| AID1330748 | Inhibition of equine serum BuChE using s-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1338133 | Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis, in-silico and biological evaluation of novel donepezil derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1872724 | Inhibition of human recombinant MAO-B incubated for 30 mins by fluorescence based assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy. |
| AID1261746 | Cognitive enhancing effect in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as time spent in effective region at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by Morris water maze assay ( | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1416356 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 to 3 mins time interval by Ellman's method | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1261770 | Neuroprotective activity in Wistar rat amyloid beta-induced Alzheimer's disease model assessed as reduction of dead neurons in CA2 region of hippocampus at 2 mg/kg/day administered as intragastric infusion for 32 days measured 24 hrs post last dose by hem | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1444082 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-aggregation at 25 uM after 24 hrs by thioflavin-T fluorescence assay relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1632237 | Antioxidant activity against scopolamine-induced nitrergic stress in cytosolic fraction of Albino LACA mouse brain assessed as nitrite levels at 1 mg/kg, ip by Greiss assay (Rvb = 525.49 +/- 23.26 ug/ml) | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19 | Coumarin derivatives as potential inhibitors of acetylcholinesterase: Synthesis, molecular docking and biological studies. |
| AID1694875 | Inhibition of recombinant human MAO-B using p-tyramine as substrate preincubated with enzyme for 15 mins followed incubation with substrate for 20 mins by Amplex red reagent based fluorescence based analysis | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1553353 | Inhibition of equine serum BChE using butyrylcholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins under dark condition by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18 | Microwave-Assisted Organic Synthesis, structure-activity relationship, kinetics and molecular docking studies of non-cytotoxic benzamide derivatives as selective butyrylcholinesterase inhibitors. |
| AID1723542 | Inhibition of recombinant human AChE using ATC as substrate by DTNB-reagent based Ellman's method | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | MicroRNA-Based Multitarget Approach for Alzheimer's Disease: Discovery of the First-In-Class Dual Inhibitor of Acetylcholinesterase and MicroRNA-15b Biogenesis. |
| AID282009 | Selectivity for human BChE over human AChE | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties. |
| AID1674979 | Permeability of compound by PAMPA-BBB assay | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Discovery of biphenyl pyrazole scaffold for neurodegenerative diseases: A novel class of acetylcholinesterase-centered multitargeted ligands. |
| AID1517857 | Inhibition of human AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1176160 | Inhibition of human recombinant MDR1 in cell membrane fraction preincubated for 5 mins at 1 uM measured after 40 mins by Pgp-Glo luciferase assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein. |
| AID1389181 | Inhibition of equine serum BuChE using S-butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease. |
| AID1317853 | Inhibition of equine serum BuChE preincubated for 5 mins followed by addition of butyrylthiocholine iodide as substrate measured after 2 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID1378354 | Inhibition of BACE1 (unknown origin) | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates. |
| AID1702425 | Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at IC50 using diluted compound relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1353378 | Cytotoxicity against human PBMC assessed as inhibition of cell viability after 6 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti-alzheimer prototype drug candidates. |
| AID1335939 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1517854 | Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity preincubated for 15 mins followed by AAPH addition measured every minute for 120 mins by ORAC fluorescein assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1820946 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 15 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1545271 | Inhibition of human acetylcholinesterase | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1465301 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID262756 | Selectivity for AChE over BChE | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
| AID1330782 | Hepatotoxicity in scopolamine-induced memory deficit Kunming mouse model assessed as increase in number of inflammatory cells in portal fields of liver at 5 mg/Kg, po for 6 days by hematoxylin and eosin-staining based microscopic analysis | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID748748 | Antiamnesic activity in Charles Foster albino rat assessed as reduction in scopolamine-induced increase in transfer latency at 10 mg/kg, po administered for 7 days measured 30 mins post last dose by elevated plus maze task (Rvb = 67.67 +/- 0.88 s) | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10 | Design, synthesis and evaluation of some new 4-aminopyridine derivatives in learning and memory. |
| AID1815190 | Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate by Ellman's method | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID1193155 | Inhibition of human recombinant AChE pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents. |
| AID345206 | Inhibition of human serum BChE by Ellman's assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer. |
| AID1506093 | Cognitive enhancing effect in Balb/c mouse assessed as protection against amyloid beta (1 to 42) oligomers-induced memory damage at 10 mg/kg, po qd via gavage for 17 days starting from 24 hrs post amyloid beta (1 to 42) oligomer treatment measured on day | 2018 | Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15 | Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile. |
| AID1764088 | Antiinflammatory activity in mouse microglial SIM-A9 cells assessed as reduction in LPS-stimulated nitric oxide release at 1 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | The structural simplification of lysergic acid as a natural lead for synthesizing novel anti-Alzheimer agents. |
| AID1627647 | Displacement of [3H]Nalpha-methylhistamine from human full length recombinant histamine H3 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands. |
| AID1055211 | Antioxidant activity assessed as hydrogen peroxide scavenging activity after 10 hrs by FOX assay | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID1668320 | Inhibition of LPS-induced NO release in human BV2 cells at 20 ug/ml preincubated for 4 hrs followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay | 2020 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 30, Issue:12 | Betulin isolated from Pyrola incarnata Fisch. inhibited lipopolysaccharide (LPS)-induced neuroinflammation with the guidance of computer-aided drug design. |
| AID635814 | Inhibition of BACE1 at 20 ug/mL by FRET assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID454344 | Selectivity ratio of IC50 for BChE in rat serum to IC50 for AChE in rat cortex | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors. |
| AID1400276 | Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 10 uM after 48 hrs by thioflavin-T fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
| AID1465285 | Inhibition of human serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | 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. |
| AID1225693 | Selectivity index, ratio of IC50 for rat serum BuChE to IC50 for rat cortex AChE | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1338134 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis, in-silico and biological evaluation of novel donepezil derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease. |
| AID1416357 | Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 to 3 mins time interval by Ellman's method | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 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. |
| AID1339461 | Cognition enhancement activity in Charles Foster albino rat model of spatial working memory assessed as escape latency at 10 mg/kg, po for administered from day 1 to 10 measured 1 hr post last dose on day 10 by Morris water maze test (Rvb = 14.12 +/- 0.78 | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1506841 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by spectroscopy based Ellman's method | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Rational design, synthesis and biological screening of triazine-triazolopyrimidine hybrids as multitarget anti-Alzheimer agents. |
| AID1319303 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 10 and 30 uM measured after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18 | Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. |
| AID1220554 | Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
| AID1253475 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors. |
| AID1772659 | In vivo inhibition of AChE in ICR mouse brain at 10 mg/kg, po measured after 1.5 hrs by Ellman method relative to control | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID658005 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 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. |
| AID1695768 | Neurotoxicity against human SH-SY5Y cells assessed as inhibition of cell viability incubated for 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Design and development of novel N-(pyrimidin-2-yl)-1,3,4-oxadiazole hybrids to treat cognitive dysfunctions. |
| AID1545059 | Inhibition of equine serum BuChE pre-incubated for 5 mins before butyrylthiocholine iodide substrate addition and measured after 15 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Design, synthesis, and biological evaluation of novel 4-oxobenzo[d]1,2,3-triazin-benzylpyridinum derivatives as potent anti-Alzheimer agents. |
| AID1702416 | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease. |
| AID1738141 | Ex vivo antioxidant activity in brain of scopolamine-induced Swiss albino mouse model of amnesia assessed as decrease in MDA level at 5 mg/kg, po administered for 7 days and observed after 30 mins before scopolamine treatment and measured after 15 mins | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease. |
| AID1186312 | Inhibition of AChE in rat cortex homogenates using acetylthiocholine iodide substrate incubated for 15 mins by UV spectroscopy based Ellman's method | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy. |
| AID1478779 | Antioxidant activity assessed as trolox equivalents of DPPH radical scavenging activity at 25 uM after 30 mins by UV-vis spectrophotometry | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. |
| AID1384010 | Inhibition of human AChE-mediated amyloid beta aggregation at 100 uM relative to control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
| AID1162593 | Antagonism of scopolamine-induced passive avoidance in Wistar rat assessed as latency of visiting dark box measured for 5 mins at 1 mg/kg, po dosed 30 mins after scopolamine challenge and measured 1 hr post dose | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | 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. |
| AID1076175 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 25 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1484828 | Inhibition of human erythrocyte AChE induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by ThT-based fluorometric method relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1865085 | Inhibition of human recombinant BuChe using butyrylthiocholine iodide as substrate incubated for 10 mins by DTNB reagent based Ellman's method | |||
| AID1076775 | Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 100 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 2 | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6 | Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease. |
| AID1709521 | Anti-VaD activity against BCCAO-induced Sprague-Dawley rat model of spatial memory deficit assessed as improvement in spatial learning and memory by measuring reduction in escape latency at 1 mg/kg, ig administered for 2 weeks followed by surgery and subs | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Twin drug design, synthesis and evaluation of diosgenin derivatives as multitargeted agents for the treatment of vascular dementia. |
| AID1378883 | Selectivity index, ratio of IC50 for human serum BuChE to IC50 for human AChE | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1195740 | Inhibition of human MAO-A expressed in baculovirus infected BTI insect cells preincubated for 15 mins | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | 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. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1436057 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease. |
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1152947 | Cognitive enhancing effect in C57BL/6J mouse assessed as reversal of scopolamine-induced long-term memory deficit by measuring latency time during training session at 1 mg/kg, iv administered 90 mins prior to scopolamine-challenge measured after 24 hrs by | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease. |
| AID1400283 | Reversal of scopolamine-induced memory impairment in albino Wistar rat assessed as increase in time spent in target quadrant in probe day at 2.5 mg/kg, ip by Morris water maze test | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
| AID752341 | Displacement of [3H]DTG from sigma 1 receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10 | Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
| AID1501299 | Metal chelating activity assessed as inhibition of Cu2+ mediated human amyloid beta (1 to 40) aggregation at 25 uM after 2 hrs by turbidity assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1279137 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID1230938 | Inhibition of human recombinant MAO-A using kynuramine substrate at 10 uM by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14 | Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases. |
| AID1421884 | Selectivity index, ratio of IC50 for human serum BuChE to IC50 for human AChE | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors. |
| AID1568789 | Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as susbtrate preincubated for 6 mins followed by substrate addition measured up to 3 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1673629 | Ex vivo inhibition of AChE in brain of scopolamine-induced Wistar rat model of amnesia at 5 mg/kg, po pretreated for 7 days followed by scopolamine challenge and measured after 30 mins using acetylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 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. |
| AID1421279 | Inhibition of electric eel AChE at 50 uM using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents. |
| AID635872 | Selectivity ratio of IC50 for equine serum BuchE to IC50 for Electrophorus electricus AchE | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | 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 di |
| AID1077081 | Inhibition of Cu2+-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM after 24 hrs by thioflavin T fluorescence method | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1444070 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate measured after 15 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1498421 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured after 20 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis, structure-activity relationship and molecular docking studies of 3-O-flavonol glycosides as cholinesterase inhibitors. |
| AID1330755 | Selectivity index, ratio of IC50 for human serum BuChE to IC50 for human erythrocyte AChE | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1501302 | Inhibition of 59Fe2+ uptake from transferrin in human SK-N-MC cells labeled with 59Fe2-Tf assessed as 59Fe uptake level at 25 uM after 3 hrs by gamma scintillation counting method relative to untreated control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1478774 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate pretreated for 6 mins followed by substrate addition measured up to 180 sec by Ellman's method | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. |
| AID1552586 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 6 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1484817 | Selectivity index, ratio of IC50 for rat serum BuChE to IC50 for rat cortex homogenate AChE | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis and evaluation of scutellarein-O-acetamidoalkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID763848 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins prior to substrate addition by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1261722 | Metabolic stability in rat liver microsomes after 5 to 180 mins by HPLC-UV analysis | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease. |
| AID1225691 | Inhibition of BuChE in rat serum using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1632238 | Inhibition of acetylcholinesterase in Albino LACA mouse brain homogenates using acetylthiocholine iodide as substrate measured for 2 mins by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19 | Coumarin derivatives as potential inhibitors of acetylcholinesterase: Synthesis, molecular docking and biological studies. |
| AID1556049 | Inhibition of electric eel AChE assessed as reduction in production of H202 using acetylcholine as substrate incubated for 15 mins followed by substrate addition by horse radish peroxidase/Amplex red reagent based fluorescence assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Dipropargyl substituted diphenylpyrimidines as dual inhibitors of monoamine oxidase and acetylcholinesterase. |
| AID695010 | Antialzheimer activity in Kunming mouse assessed as reversal of amyloid beta (1 to 42)-induced decrease of swimming percentage of path length at 0.656 mg/kg, po qd measured on day 13 by morris water maze test | 2012 | ACS medicinal chemistry letters, Nov-08, Volume: 3, Issue:11 | Identification of aminopyridazine-derived antineuroinflammatory agents effective in an Alzheimer's mouse model. |
| AID1351940 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured every minute for 10 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine "bio-oxidizable" prodrugs: Synthesis, biological evaluation and structure-activity relationship. |
| AID635870 | Inhibition of Electrophorus electricus AchE using acetylthiocholine iodide as substrate preincubated for 10 mins measured after 15 mins of substrate addition by Ellman's method | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | 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 di |
| AID1772665 | Improvement in learning and spatial memory in amyloid beta (1 to 42)-induced mouse model of Alzheimer's disease at 10 mg/kg/day, po pretreated with amyloid beta42 for 3 days followed by treatment with compound and measured after 9 days measured by Y-maze | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in th |
| AID1596166 | Noncompetitive inhibition of electric eel AChE assessed as effect on Km of substrate at 12.5 nM to 50 nM using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured for 5 mins by double reciprocal Lineweaver-Bu | 2019 | European journal of medicinal chemistry, Jul-15, Volume: 174 | Benzoic acid-derived nitrones: A new class of potential acetylcholinesterase inhibitors and neuroprotective agents. |
| AID1631819 | Inhibition of equine BuChE using ACTI as substrate preincubated for 29 mins followed by substrate addition measured at 1 min intervals for 10 mins by Ellman's assay | 2016 | Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16 | Discovery and Structure-Activity Relationships of a Highly Selective Butyrylcholinesterase Inhibitor by Structure-Based Virtual Screening. |
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| AID1217705 | Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
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| AID763833 | Activity at AChE in Charles Foster rat hypothalamus assessed as substrate hydrolyzed per mg of protein at 10 mg/kg, po for 8 days by Ellman's method (Rvb = 40.50 +/- 0.76 mol/min) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents. |
| AID1818855 | Cognitive enhancing effect in Wistar rat model of scopolamine-induced working memory impairment assessed as reduction in number of working memory errors at 5 mg/kg by Radial arm maze task | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Designed Peptide Inhibitors of STEP Phosphatase-GluA2 AMPA Receptor Interaction Enhance the Cognitive Performance in Rats. |
| AID1379017 | Selectivity index, ratio of IC50 for human serum BChE to IC50 for human erythrocytic AChE | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1406251 | Inhibition of AChE (unknown origin) | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities. |
| AID1824579 | Inhibition of AChE in mouse cortical homogenate using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1552587 | Inhibition of human plasma BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured at 6 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, β-amyloid aggregation and oxidative stress to treat Alzheimer's disease. |
| AID1330753 | Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1537665 | Neuroprotective activity against amyloid beta (1 to 42)-induced cytotoxicity in human SH-SY5Y cells assessed as cell viability at 10 uM preincubated for 3 hrs followed by amyloid beta (1 to 42) addition and measured after 24 hrs by MTT assay (Rvb = 78 +/- | 2019 | MedChemComm, Jun-01, Volume: 10, Issue:6 | Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
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| AID1322902 | Inhibition of human recombinant BuChE expressed in HEK293 cells using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation. |
| AID1459558 | Inhibition of recombinant human MAO-A assessed as reduction in 4-hydroxyquinolone production using kynuramine as substrate after 20 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1581642 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | 1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease. |
| AID1633170 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease. |
| AID1704818 | Inhibition of recombinant human AChE using ATCI as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method | |||
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| AID1698413 | Inhibition of human BACE-1 by FRET assay | 2020 | Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22 | Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease. |
| AID1867626 | Inhibition of human AChE by Ellman's spectrophotometric method | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease. |
| AID30541 | Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in electric eel | 1998 | Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6 | Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase. |
| AID1055866 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2013 | European journal of medicinal chemistry, , Volume: 70 | Novel coumarin-3-carboxamides bearing N-benzylpiperidine moiety as potent acetylcholinesterase inhibitors. |
| AID1609214 | Cognitive enhancing effect in scopolamine-induced Wistar rat model of amnesia assessed as increase in spontaneous alteration at 5 mg/kg pretreated for 7 days followed by scopolamine challenge and measured after 30 mins by Y-maze test | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine derivatives as multi-target directed ligands for the treatment of Alzheimer's disease. |
| AID1230940 | Inhibition of human recombinant MAO-B using kynuramine substrate at 10 uM by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14 | Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases. |
| AID1707769 | Antiinflammatory activity in LPS-induced human THP-1 cells assessed as reduction in nitric oxide release at 10 uM peincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease. |
| AID1906377 | Inhibition of electric eel AChE-induced amyloid beta42 aggregation at 0.001 to 5 uM measured after 24 hrs by ThioflavinT-dye based fluorescence analysis | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. |
| AID1694871 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 6 mins followed by substrate addition and measured for 180 secs by Ellman's method | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease. |
| AID1383664 | Inhibition of electric eel AChE-induced amyloid beta (1 to 42) aggregation at 10 uM after 48 hrs by thioflavin T fluorescence spectroscopic method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
| AID1884589 | Neuroprotective activity against rat PC-12 cells assessed as inhibition of Abeta(25-35)-induced cytotoxicity by measuring increase in cell viability at 10 uM incubated for 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease. |
| AID600978 | Inhibition of human erythrocytes AChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID1339441 | Selectivity index, ratio of IC50 for horse serum BuChE to IC50 for electric eel AChE | 2017 | Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4 | Design, synthesis and evaluation of some N-methylenebenzenamine derivatives as selective acetylcholinesterase (AChE) inhibitor and antioxidant to enhance learning and memory. |
| AID1220558 | Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
| AID1801604 | AChE Inhibition Assay from Article 10.1016/j.bioorg.2015.12.002: \\Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.\\ | 2016 | Bioorganic chemistry, Apr, Volume: 65 | Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives. |
| AID1801892 | Anticholinesterase Enzyme Inhibition Assay from Article 10.1016/j.bioorg.2016.05.002: \\Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.\\ | 2016 | Bioorganic chemistry, 08, Volume: 67 | Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies. |
| AID1796570 | Cholinesterase Inhibition Assay from Article 10.1021/jm0340602: \\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 | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | 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. |
| AID1796269 | Measurement of FBSAChE/EqBuChE Inhibitory Activity from Article 10.1021/jm049510k: \\Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design o | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. |
| AID1802170 | AChE and BuChE Inhibition Assay from Article 10.1111/cbdd.12822: \\Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease.\\ | 2016 | Chemical biology & drug design, Dec, Volume: 88, Issue:6 | Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease. |
| AID1802055 | In vitro AChE and BChE Assay from Article 10.1016/j.bioorg.2016.10.002: \\Rational design and synthesis of dihydropyrimidine based dual binding site acetylcholinesterase inhibitors.\\ | 2016 | Bioorganic chemistry, 12, Volume: 69 | Rational design and synthesis of dihydropyrimidine based dual binding site acetylcholinesterase inhibitors. |
| AID1802171 | Monoamine Oxidase Assay from Article 10.1111/cbdd.12822: \\Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease.\\ | 2016 | Chemical biology & drug design, Dec, Volume: 88, Issue:6 | Evaluation of multifunctional synthetic tetralone derivatives for treatment of Alzheimer's disease. |
| AID1796282 | Cholinesterase Inhibition Assay from Article 10.1016/j.bmc.2005.09.029: \\Donepezil-tacrine hybrid related derivatives as new dual binding site inhibitors of AChE.\\ | 2005 | Bioorganic & medicinal chemistry, Dec-15, Volume: 13, Issue:24 | Donepezil-tacrine hybrid related derivatives as new dual binding site inhibitors of AChE. |
| AID1796482 | Cholinesterase Inhibition Assay from Article 10.1021/jm050578p: \\Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.\\ | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
| AID1801483 | AChE and BChE Inhibitory Activities from Article 10.1016/j.bioorg.2015.09.009: \\Synthesis, cholinesterase inhibition and molecular modelling studies of coumarin linked thiourea derivatives.\\ | 2015 | Bioorganic chemistry, Dec, Volume: 63 | Synthesis, cholinesterase inhibition and molecular modelling studies of coumarin linked thiourea derivatives. |
| AID1802649 | Cholinesterases Inhibition Assay from Article 10.1111/cbdd.12902: \\Synthesis and anticholinesterase activity of new substituted benzo[d]oxazole-based derivatives.\\ | 2017 | Chemical biology & drug design, 05, Volume: 89, Issue:5 | Synthesis and anticholinesterase activity of new substituted benzo[d]oxazole-based derivatives. |
| AID1803321 | Enzymatic Assay from Article 10.3109/14756366.2012.709242: \\Design, synthesis and evaluation of new thiazole-piperazines as acetylcholinesterase inhibitors.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Oct, Volume: 28, Issue:5 | Design, synthesis and evaluation of new thiazole-piperazines as acetylcholinesterase inhibitors. |
| AID1801407 | AChE and BChE Inhibition Assay from Article 10.1111/cbdd.12579: \\Syntheses, cholinesterases inhibition, and molecular docking studies of pyrido[2,3-b]pyrazine derivatives.\\ | 2015 | Chemical biology & drug design, Nov, Volume: 86, Issue:5 | Syntheses, cholinesterases inhibition, and molecular docking studies of pyrido[2,3-b]pyrazine derivatives. |
| AID1796572 | Cholinesterase Inhibition Assay from Article 10.1021/jm010491d: \\Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.\\ | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
| AID1802598 | AChE/BuChE Inhibition Assay from Article 10.1016/j.bioorg.2017.02.016: \\Pyridoxine-resveratrol hybrids Mannich base derivatives as novel dual inhibitors of AChE and MAO-B with antioxidant and metal-chelating properties for the treatment of Alzheimer's | 2017 | Bioorganic chemistry, 04, Volume: 71 | Pyridoxine-resveratrol hybrids Mannich base derivatives as novel dual inhibitors of AChE and MAO-B with antioxidant and metal-chelating properties for the treatment of Alzheimer's disease. |
| AID1801052 | Cholinesterase Inhibition Assay from Article 10.1016/j.bioorg.2015.05.005: \\Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis.\\ | 2015 | Bioorganic chemistry, Aug, Volume: 61 | Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis. |
| AID1803295 | AChE and BuChE Activity Assay from Article 10.3109/14756366.2012.688041: \\Synthesis and anticholinesterase activities of novel 1,3,4-thiadiazole based compounds.\\ | 2013 | Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 28, Issue:4 | Synthesis and anticholinesterase activities of novel 1,3,4-thiadiazole based compounds. |
| AID1801534 | AChE and BChE Inhibition Activity from Article 10.1016/j.bioorg.2016.01.004: \\One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.\\ | 2016 | Bioorganic chemistry, Apr, Volume: 65 | One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies. |
| AID1802080 | Cholinesterase Inhibition Assay from Article 10.1111/cbdd.12800: \\Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease.\\ | 2016 | Chemical biology & drug design, 11, Volume: 88, Issue:5 | Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease. |
| AID1799797 | Inhibition Assay from Article 10.1111/j.1747-0285.2012.01435.x: \\Synthesis and Biological Evaluation of 3-thiazolocoumarinyl Schiff-base Derivatives as Cholinesterase Inhibitors.\\ | 2012 | Chemical biology & drug design, Oct, Volume: 80, Issue:4 | Synthesis and biological evaluation of 3-thiazolocoumarinyl Schiff-base derivatives as cholinesterase inhibitors. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID1345946 | Human acetylcholinesterase (Cartwright blood group) (Hydrolases) | 1994 | European journal of pharmacology, Apr-04, Volume: 270, Issue:2-3 | Acetylcholinesterase protection and the anti-diisopropylfluorophosphate efficacy of E2020. |
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| AID1345946 | Human acetylcholinesterase (Cartwright blood group) (Hydrolases) | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | QSAR analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase. |
| AID493017 | Wombat Data for BeliefDocking | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 180 (5.95) | 18.2507 |
| 2000's | 1128 (37.28) | 29.6817 |
| 2010's | 1243 (41.08) | 24.3611 |
| 2020's | 475 (15.70) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (116.78) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 557 (17.44%) | 5.53% |
| Reviews | 446 (13.97%) | 6.00% |
| Case Studies | 259 (8.11%) | 4.05% |
| Observational | 20 (0.63%) | 0.25% |
| Other | 1,911 (59.85%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Phase III Double Blind, Placebo Controlled Study of Donepezil in the Irradiated Brain [NCT00369785] | Phase 3 | 198 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| A Phase II Double-blind, Randomized, Placebo-controlled, Parallel-group Study to Evaluate the Efficacy and Safety of STA-1 as an Add-on Treatment to Donepezil in Patients With Mild to Moderate Alzheimer's Disease [NCT01255046] | Phase 2 | 136 participants (Anticipated) | Interventional | 2015-12-31 | Not yet recruiting | ||
| A Randomized, Double-Blind, Sponsor Unblinded, Placebo- And Positive- Controlled Study To Evaluate The Effects Of Single Oral Administrations Of PF-04995274, Alone Or In Combination With Donepezil, On Scopolamine-Induced Deficits In Psychomotor And Cognit [NCT01345864] | Phase 1 | 88 participants (Actual) | Interventional | 2011-05-31 | Terminated(stopped due to See termination reason in detailed description.) | ||
| Evaluation of Safety and Pharmacokinetic Profiles of a Single-dose HHT201 in Healthy Subjects [NCT03932916] | Phase 1 | 38 participants (Actual) | Interventional | 2019-07-02 | Completed | ||
| Post-marketing Surveillance of Long-term Administration of Donepezil Hydrochloride -Investigation of the Clinical Condition and Safety in Patients With Alzheimer's Disease- [NCT01129596] | 10,238 participants (Actual) | Observational | 2010-06-10 | Completed | |||
| A Randomized, Double-Blinded Clinical Trial to Assess the Safety, Tolerability and Pharmacokinetics of MK-4334 in Participants With Alzheimer's Clinical Syndrome on a Stable Dose of Donepezil [NCT03740178] | Phase 1 | 12 participants (Anticipated) | Interventional | 2019-09-27 | Not yet recruiting | ||
| A Five-Period, Placebo-Controlled, Crossover Study to Evaluate the Effect of Donepezil and MK-3134 on Reversal of Cognitive Impairment Associated With a Single-Dose of Scopolamine. [NCT01181310] | Phase 1 | 31 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| Evaluation of Three Potential CNS Pretreatments for Soman Exposure - Huperzine A, Donepezil, and Galantamine - on Human Performance [NCT01194336] | 84 participants (Actual) | Observational | 2012-02-29 | Completed | |||
| A Double-Blind, Placebo-Controlled Evaluation of The Efficacy and Safety of AChE Inhibitor Donepezil As Adjunctive Treatment to Mood Stabilizers in Acute Mania [NCT01191918] | Phase 4 | 40 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
| A Randomized, Double-Blind, Sponsor Unblinded, Placebo-Controlled, 5-Period Crossover, Phase 1b Study To Evaluate The Effects Of Single Oral Administration of TAK-071 On Scopolamine-Induced Cognitive Impairment In Healthy Subjects [NCT02918266] | Phase 1 | 18 participants (Actual) | Interventional | 2016-11-21 | Terminated(stopped due to Terminated prematurely due to indication change.) | ||
| The Effect of Donepezil in Radiotherapy-related Cognitive Impairment: a Randomized, Double-blind, Placebo-controlled Clinical Trial [NCT03907371] | Phase 2 | 238 participants (Anticipated) | Interventional | 2019-05-01 | Recruiting | ||
| A Phase III, Multicenter, Randomized, Double-blind, Positive /Placebo Controlled, Parallel, Three Arms Study of Tianzhi Granule in Mild to Moderate Vascular Dementia [NCT02453932] | Phase 3 | 543 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| A Multinational, Multi-center, Randomized, Double-blind, Active Comparator, Phase III Clinical Trial to Evaluate the Efficacy and Safety of Donepezil Transdermal Patch in Patients With Alzheimer's Disease [NCT03197740] | Phase 3 | 399 participants (Actual) | Interventional | 2017-10-12 | Completed | ||
| Post-marketing Surveillance of Donepezil Hydrochloride - Investigation of Long Term Safety and Efficacy of Aricept as Well as Its Proper Use Information in Patients With Dementia With Lewy Bodies. [NCT02448784] | 591 participants (Actual) | Observational | 2015-04-20 | Completed | |||
| A Multidisciplinary Approach to Manage Gait Difficulty in Parkinson Patients [NCT02857244] | Phase 2 | 0 participants (Actual) | Interventional | 2016-11-30 | Withdrawn(stopped due to Site did not obtain LIRB approval due to medication usage.) | ||
| An Open-label Study to Evaluate the Safety of Donepezil Hydrochloride((Aricept®) for up to 1 Year in the Treatment of Cognitive Dysfunction Exhibited by Children With Down Syndrome-Follow-up to a 10-Week,Double-Blind,Placebo-Controlled Trial [NCT00675025] | Phase 2 | 117 participants (Actual) | Interventional | 2008-04-04 | Terminated(stopped due to Sufficient evidence of efficacy not met. Discontinuation not based on any safety concerns.) | ||
| Assessment of Cholinergic and Cognitive Function Using Pharmacologic ASL-Perfusion MRI [NCT01379001] | 60 participants (Actual) | Interventional | 2008-07-31 | Completed | |||
| Maintenance Therapies in Late-Life Depression: MTLD III [NCT00177671] | Phase 4 | 220 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
| Randomized, Double-Blind, Placebo-Controlled Study of Efficacy and Safety of Donepezil Hydrochloride in Preadolescent and Adolescent Children With Attention Impairment Following Cancer Treatment [NCT00688376] | Phase 3 | 72 participants (Actual) | Interventional | 2008-07-02 | Completed | ||
| A Discontinuation of Cholinesterase Inhibitors for the Treatment of Severe Alzheimer's Disease in Long Term Care Setting [NCT02035982] | Phase 3 | 40 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A Phase 2 Clinical Study to Explore the Optimal Dosage/Administration of PM012 Tablet in Alzheimer's Disease: Double-Blind, Randomized Between Placebo Control Group and Dose Groups, Parallel-Design, Multicenter Study [NCT05811000] | Phase 2/Phase 3 | 312 participants (Anticipated) | Interventional | 2020-11-27 | Recruiting | ||
| A Plan on Investigation and Collection of Aricept Safety Information With a Dose Increase on Alzheimer's Disease Patients [NCT02158910] | 2,231 participants (Actual) | Observational | 2015-03-31 | Completed | |||
| [NCT02162264] | 8,662 participants (Actual) | Observational | 2013-06-01 | Completed | |||
| Open Label, Randomized, Single-dose, Crossover Study to Evaluate the Pharmacokinetic Characteristics of Donepezil Between Two Donepezil Products, Aricept® Tablet and Neuropezil ODT, in Healthy Subjects [NCT01297036] | Phase 1 | 22 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| The Effect of Donepezil on Wound Healing [NCT04505670] | Phase 2 | 20 participants (Anticipated) | Interventional | 2020-08-30 | Recruiting | ||
| Four-site, Randomized, Parallel Design, Double-blind, Placebo-controlled, 10-week Trial of Donepezil 10 mg Daily for Verbal Memory Problems Among Adults With TBI in the Subacute or Chronic Recovery Period [NCT02255799] | Phase 3 | 160 participants (Anticipated) | Interventional | 2013-09-01 | Active, not recruiting | ||
| A Phase 1b, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Study to Determine the Safety, Tolerability, Pharmacokinetics, and Brain Metabolic Response, Using FDG-PET, Following Administration of AGN-242071 Added to Standard-of-C [NCT03316898] | Phase 1 | 0 participants (Actual) | Interventional | 2018-09-30 | Withdrawn(stopped due to Business decision to stop the study.) | ||
| Effects of Donepezil on Regional Cerebral Blood Flow Following Aneurysmal Subarachnoid Haemorrhage [NCT02222727] | Phase 2 | 19 participants (Actual) | Interventional | 2014-01-31 | Terminated(stopped due to CT scanner software incompatible) | ||
| A Multinational, Multicenter, Randomized, Double-blind, Parallel-group, Placebo-controlled Study of the Effect on Cognitive Performance, Safety, and Tolerability of SAR110894D at the Doses of 0.5 mg, 2 mg, and 5 mg/Day for 24 Weeks in Patients With Mild t [NCT01266525] | Phase 2 | 291 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| A Randomized, Double-Blind, Active- and Placebo-Controlled Study to Evaluate the Efficacy and Safety of ABT-288 in Subjects With Mild-to-Moderate Alzheimer's Disease [NCT01018875] | Phase 2 | 242 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
| A Randomized, Double-Blind, Placebo- and Active-Controlled, Parallel Group Study to Evaluate the Efficacy and Safety of ABT-126 in Subjects With Mild-to-Moderate Alzheimer's Disease [NCT00948909] | Phase 2 | 274 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| A Study to Assess the Steady-State Bioequivalence of Once-Weekly Corplex™ 10mg Donepezil Transdermal Delivery System Compared to Daily Oral Administration of Aricept® [NCT03259958] | Phase 1 | 86 participants (Actual) | Interventional | 2017-10-30 | Completed | ||
| [NCT02450786] | Phase 2 | 80 participants (Actual) | Interventional | 2015-06-30 | Active, not recruiting | ||
| The Efficacy of 23mg Versus 10mg of Donepezil in ParkInson's Disease With Dementia [NCT02415062] | Phase 2 | 150 participants (Anticipated) | Interventional | 2015-07-31 | Recruiting | ||
| Efficiency of Donepezil in Elderly Patients Undergoing Orthopedic Surgery Due to Underlying Postoperative Cognitive Dysfunction, a Multicenter Randomized Controlled Trial [NCT04423276] | Phase 4 | 360 participants (Anticipated) | Interventional | 2020-06-14 | Recruiting | ||
| A Phase 1, Crossover Study to Evaluate the Pharmacokinetics of Corplex™ Donepezil 10 mg Transdermal Delivery System Applied to Different Body Locations [NCT03432195] | Phase 1 | 66 participants (Actual) | Interventional | 2018-01-31 | Completed | ||
| A Double Blind, Placebo-controlled, Randomized, 15-day Treatment, Pharmacodynamics, Safety, and Pharmacokinetics Study of THN201 Versus Donepezil Administered Orally to Healthy Male Volunteers Including a Scopolamine Challenge [NCT03698695] | Phase 1 | 152 participants (Actual) | Interventional | 2018-09-27 | Completed | ||
| A Randomized Double-Blind Study to Assess the Skin Irritation and Sensitization Potential of Once-Weekly Corplex™ Donepezil Transdermal Delivery System [NCT03397862] | Phase 1 | 256 participants (Actual) | Interventional | 2017-11-14 | Completed | ||
| The Effect of Electroacupuncture Combined With Donepezil on Cognitive Function in Alzheimer's Disease Patients: Study Protocol for a Randomized Controlled Trial [NCT02305836] | Phase 2 | 334 participants (Anticipated) | Interventional | 2017-06-30 | Recruiting | ||
| [NCT02178124] | Phase 1 | 24 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
| A Randomized, Double-Blind, Placebo and Active-Controlled Study to Evaluate the Efficacy and Safety of ABT-126 in Subjects With Mild to Moderate Alzheimer's Disease [NCT01527916] | Phase 2 | 438 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| A Randomized, Double-Blind, Placebo and Active-Controlled, Parallel Group Study to Evaluate the Efficacy and Safety of ABT-384 in Subjects With Mild-to-Moderate Alzheimer's Disease [NCT01137526] | Phase 2 | 267 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| Treatment With Acetyl-Choline Esterase Inhibitors in Children With Autism [NCT01098383] | Phase 4 | 84 participants (Anticipated) | Interventional | 2010-03-31 | Recruiting | ||
| A 52-week, Multicentre Open Label Extension Study of the Safety Tolerability and Efficacy of Donepezil (Aricept) in Parkinson's Disease (PD) Patients With Dementia [NCT01327859] | Phase 3 | 357 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
| A Randomized, Double-Blind, Sponsor Unblinded, Placebo Controlled, 5-Way, Crossover Study To Evaluate The Effects Of Single Oral Administrations of PF-05212377 (SAM-760), A 5-HT6 Antagonist, On Scopolamine Induced Deficits In Psychomotor And Cognitive Fun [NCT01213355] | Phase 1 | 38 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| Novel Methods for Clinical Trials in Dementia and Cognitive Decline [NCT05592678] | Phase 2/Phase 3 | 200 participants (Anticipated) | Interventional | 2023-11-30 | Not yet recruiting | ||
| A Phase II, Multi-center, Randomized, Double-blind, Placebo-controlled, Crossover Study to Evaluate the Pharmacodynamic Effect of Single and Multiple Oral Doses of AZD1446/ Placebo and a Single Dose of Donepezil on Quantified Electroencephalography and Ev [NCT01125683] | Phase 2 | 40 participants (Anticipated) | Interventional | 2010-06-30 | Terminated(stopped due to Poor recruitment.) | ||
| A Randomized, Double-Blind, Placebo-Controlled Study of the Safety and Pharmacokinetics of MK-1942 Administered to Alzheimer's Disease Patients Receiving Donepezil Treatment. [NCT04308304] | Phase 1 | 27 participants (Actual) | Interventional | 2021-02-16 | Completed | ||
| A Phase 1, 2-Way Crossover Study to Evaluate the Effect of Heat Application on the Delivery Profile of Corplex™ Donepezil 5 mg Transdermal Delivery System (TDS) in Healthy Volunteers [NCT03438604] | Phase 1 | 24 participants (Actual) | Interventional | 2018-02-13 | Completed | ||
| An Open-Label, Multicenter, One-Year Extension Of The Evaluation Of The Efficacy And Safety Of Donepezil Hydrochloride (E2020) In Migraine Prophylaxis [NCT01146509] | Phase 2 | 89 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
| A Multi-center Study for the Clinical Response of Choline Acetyltransferase and Apolipoprotein Epsilon Gene Polymorphisms to Donepezil in Alzheimer's Disease [NCT00381381] | Phase 4 | 199 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
| Alzheimer's Disease Long-term Follow-up Study (ALF Study) [NCT00165724] | Phase 4 | 114 participants (Actual) | Interventional | 2004-06-30 | Completed | ||
| Pilot Study of Sleep Therapy and Biomarkers in Children With Autism Spectrum Disorders [NCT02487082] | Phase 2 | 12 participants (Actual) | Interventional | 2015-06-30 | Terminated(stopped due to too few subjects enrolled) | ||
| A 12-Week, Multicenter, Open Label Study To Evaluate The Effectiveness And Safety Of Donepezil Hydrochloride (E2020) In Subjects With Mild To Severe Alzheimer's Disease Residing In An Assisted Living Facility [NCT00571064] | Phase 4 | 97 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| A Relative Bioavailability Study of 10 mg Donepezil Hydrochloride Orally Disintegrating Tablets Under Non-Fasting Conditions. [NCT01260948] | Phase 1 | 26 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
| MELA Study - Hedonic Study on the Taste of Drugs Crushed in Food: Observational Study Involving 16 Healthy Volunteers [NCT02570581] | Phase 1 | 16 participants (Actual) | Interventional | 2014-06-30 | Completed | ||
| Effects of Galantamine and Donépézil on the Amount and the Quality oh the Sleep in Patients Suffering From Alzheimer Disease. [NCT00750529] | Phase 1 | 15 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
| Donepezil Therapy and Changes of Symptoms and Glucose Metabolism in Patients With Dementia With Lewy Bodies (DLB) [NCT00776347] | 24 participants (Actual) | Interventional | 2008-10-31 | Completed | |||
| Clinical Evaluation on the Therapeutic Effect of Acupuncture Treatment for Alzheimer's Disease: Multicenter Randomized Controlled Trial [NCT03810794] | 180 participants (Anticipated) | Interventional | 2019-03-01 | Recruiting | |||
| Efficacy of Zydena (Udenafil) on Cognitive Function of Alzheimer's Disease Patients: A Randomized, Double Blind, Placebo-controlled Multicenter Study [NCT01940952] | Phase 3 | 210 participants (Anticipated) | Interventional | 2013-09-30 | Not yet recruiting | ||
| A Six-month, Multicenter, Double-blind, Parallel, Placebo-controlled Study of the Effect on Global/Behavioural/ADL Functions and Tolerability of Aricept in Patients Wtih Severe Alzheimer's Disease Living in an Assisted Care Facility [NCT00630851] | Phase 3 | 249 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
| A Phase 1 Safety, Tolerability, and Pharmacokinetic Study of Escalating Single and Multiple Oral Doses of TAK-071 in Healthy Subjects and Subjects With Mild Cognitive Impairment/Mild Alzheimer Disease and Relative Bioavailability and Food Effect of TAK-07 [NCT02769065] | Phase 1 | 179 participants (Actual) | Interventional | 2016-05-05 | Terminated(stopped due to Terminated prematurely as data from cohort no longer needed due to indication change.) | ||
| [NCT02055703] | Phase 1 | 195 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| Phase III Trial of Octohydroaminoacridine Succinate Tablet for Mild-to-Moderate Alzheimer's Disease: a 26 Weeks, Randomized, Double-blind, Double-dummy, Placebo- and Positive- Parallel Controlled and Extended Single Arm to 54 Weeks Multicentre Study [NCT03283059] | Phase 3 | 600 participants (Anticipated) | Interventional | 2017-08-16 | Recruiting | ||
| A Randomized, Open-label, Single Dose, Crossover Study to Evaluate the Effect of D797 on Pharmacokinetics of D324 in Healthy Volunteers [NCT03569579] | Phase 1 | 20 participants (Actual) | Interventional | 2018-04-16 | Completed | ||
| A Double-blind, Placebo-controlled Comparative Study and Open-label Extension Study to Confirm the Efficacy and Safety of E2020 in Subjects With Down Syndrome Having Regression Symptoms and Disabled Activities of Daily Living. [NCT02094053] | Phase 2 | 36 participants (Actual) | Interventional | 2013-09-12 | Completed | ||
| [NCT02162251] | 3,482 participants (Actual) | Observational | 2013-06-01 | Completed | |||
| Gastrointestinal Motility Among Diabetes Patients [NCT02573519] | 40 participants (Actual) | Interventional | 2015-10-31 | Terminated(stopped due to Renewal of PET/CT scanners and slow recruitment) | |||
| A Double-blind, Randomised, Cross-over, Placebo-controlled Study of Repeated Oral Doses of AZD3480 and a Single Dose of Donepezil to Evaluate the Pharmacokinetic Interaction Between AZD3480 and Donepezil in Healthy Extensive and Poor Metabolisers of CYP2D [NCT00713765] | Phase 1 | 33 participants (Actual) | Interventional | 2008-12-31 | Terminated(stopped due to Ended prematurely - The trial never commenced.) | ||
| A Randomised, Double-blind, Placebo-controlled, Parallel Design, Multicentre Study in Patients With Mild to Moderate Alzheimer's Disease to Investigate the Effect on Cognitive Function as Measured by Repeated CogState Testing in Relation to Effects on Tra [NCT01024660] | Early Phase 1 | 155 participants (Anticipated) | Interventional | 2009-12-31 | Completed | ||
| The Impact of Cholinesterase Inhibitors on Driving Ability in Healthy Older Adults: A Pilot Study [NCT00482001] | Phase 4 | 22 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| A Study to Investigate the Effects of Donepezil on the Pharmacokinetics of BI 425809 and Vice Versa in Healthy Male and Female Subjects (Open-label, Two-treatment, Two-period, One Fixed Sequence Cross-over Design) [NCT03905096] | Phase 1 | 32 participants (Actual) | Interventional | 2019-04-12 | Completed | ||
| A Multicenter, Randomized, Open-label, Prospective Trial to Evaluate the Safety and Tolerability of Donepezil 23 mg With or Without Intermediate Dose Titration in Patients With Alzheimer's Disease Taking Donepezil Hydrochloride 10 mg [NCT02550665] | Phase 3 | 176 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
| Comparative Assessment of Clinical Efficacy of Donepezil Between the Patients With Alzheimer's Disease and Mixed Dementia [NCT01023867] | 88 participants (Actual) | Interventional | 2007-03-31 | Completed | |||
| Can Cognitive Enhancers Reduce the Risk of Falls in Older People With Mild Cognitive Impairment? A Randomized Controled Trial [NCT00934531] | 60 participants (Actual) | Interventional | 2009-09-30 | Completed | |||
| A Phase 1, Randomized, Open-Label, Exploratory, Sequential, Pharmacokinetic Single Ascending Dose Study of IVL3003 Versus Multiple Doses of Aricept (Donepezil) Tablets in Healthy Subjects [NCT05345509] | Phase 1/Phase 2 | 42 participants (Anticipated) | Interventional | 2023-04-01 | Recruiting | ||
| Safety and Efficacy of Donepezil in Mild to Moderate Alzheimer's Disease: A Multi-center Single-arm Study in China [NCT02787746] | Phase 4 | 241 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
| A Randomized, Double-Blind, Clinical Trial to Compare the Safety and Efficacy of Cerebrolysin and Aricept (Donepezil) and a Combination Therapy in Patients With Probable Alzheimer's Disease (AD) [NCT00911807] | Phase 2 | 217 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
| Randomized, Double-blind, Placebo-controlled, Single Ascending Dose Phase 1 Clinical Trial to Evaluate Safety, Tolerability and Pharmacokinetics of DKF-310 Intramuscular Injection in Healthy Male Volunteers [NCT02695004] | Phase 1 | 44 participants (Actual) | Interventional | 2016-02-29 | Completed | ||
| A 52-Week, Two-Period, Multicenter, Randomized, Double-Blind, Donepezil-Referenced, Placebo-Controlled, Efficacy And Safety Study Of 3 Dosage Levels Of SAM-531 In Outpatients With Mild To Moderate Alzheimer Disease [NCT00895895] | Phase 2 | 526 participants (Actual) | Interventional | 2009-05-31 | Terminated(stopped due to See termination reason in detailed description.) | ||
| A Long-term, Extension Study of E2020 in Patients With Dementia With Lewy Bodies [NCT00598650] | Phase 2 | 160 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| Combined Administration Of Begacestat And Donepezil: A Multiple-Dose Study In Healthy Subjects [NCT00959881] | Phase 1 | 47 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| Telerehabilitation Combining Virtual Reality Adaptable Games and Drug Therapy for Early Alzheimer's Disease - Feasibility [NCT04732182] | 14 participants (Anticipated) | Interventional | 2022-02-16 | Recruiting | |||
| The Effect of Donepezil on Glycemic Control in Type II Diabetics [NCT04507438] | Phase 2 | 7 participants (Actual) | Interventional | 2019-07-12 | Terminated(stopped due to Lack of enrollment) | ||
| Open-Label Extension Study of 23 mg Donepezil SR in Patients With Moderate to Severe Alzheimer's Disease [NCT00566501] | Phase 3 | 915 participants (Actual) | Interventional | 2007-12-14 | Completed | ||
| A Single-blinded, Placebo- and Active-controlled, Parallel, Single-ascending Dose Phase 1 Clinical Trial to Evaluate the Safety and Pharmacokinetics of DA-5207 Transdermal Delivery System in Healthy Adults [NCT04013477] | Phase 1 | 40 participants (Actual) | Interventional | 2019-06-18 | Completed | ||
| Multi-centre UK Study of the Acetylcholinesterase Inhibitor Donepezil in Early Dementia Associated With Parkinson's Disease [NCT01014858] | Phase 3 | 64 participants (Actual) | Interventional | 2013-01-31 | Terminated(stopped due to Due to low recruitment) | ||
| A 54-week, Double-blind, Randomized, Placebo-controlled, Parallel-group Study to Investigate the Effects of Rosiglitazone (Extended Release Tablets) as Adjunctive Therapy to Donepezil on Cognition and Overall Clinical Response in APOE ε4-stratified Subjec [NCT00348309] | 1,496 participants (Actual) | Interventional | 2006-07-06 | Completed | |||
| Post-marketing Surveillance of Donepezil Hydrochloride- Investigation of the Clinical Safety and Effectiveness in Patients With Alzheimer's Disease [NCT01251718] | 894 participants (Actual) | Observational | 2010-12-01 | Completed | |||
| An 18-Week, Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study Of The Efficacy, Safety, And Tolerability Of Donepezil HCl (E2020) In Patients With CADASIL Who Have Cognitive Impairment [NCT00103948] | Phase 2 | 165 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Trial, With Placebo Run-In, and an Open-Label Treatment Period, to Evaluate the Performance of the CogState Computerized Neuropsychological Battery and the ADAS-Cog in Generally C [NCT00777608] | Phase 1 | 106 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| A 10-Week, Double-Blind, Placebo-Controlled Study To Evaluate The Efficacy And Safety Of Donepezil Hydrochloride (Aricept) In The Treatment Of The Cognitive Dysfunction Exhibited By Children With Down Syndrome, Aged 11 To 17 [NCT00754052] | Phase 3 | 8 participants (Actual) | Interventional | 2008-09-30 | Terminated(stopped due to Sufficient evidence of efficacy not met. Discontinuation not based on any safety concerns.) | ||
| Pathogenesis of Rett Syndrome: Natural History and Treatment [NCT00069550] | Phase 3 | 90 participants | Interventional | 2004-09-30 | Recruiting | ||
| Detecting an Early Response to Donepezil With Measures of Visual Attention [NCT03073876] | Phase 4 | 25 participants (Actual) | Interventional | 2005-12-01 | Completed | ||
| The Neural and Behavioral Correlates of How Donepezil Modulates Memory and Inhibitory Efficiency in the Context of 24 Hours of Sleep Deprivation [NCT00800553] | Phase 4 | 43 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
| Augmentation of the Cholinergic System in Fragile X Syndrome: A Double-Blind Placebo-Controlled Randomized Study of Donepezil [NCT01120626] | Phase 2 | 45 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| A Study of Cholinergic Augmentation in Frequently Falling Subjects With Parkinson's [NCT00912808] | 23 participants (Actual) | Interventional | 2005-10-31 | Completed | |||
| A 12-Week, Double-Blind, Placebo-Controlled Study To Evaluate The Impact Of Donepezil Hydrochloride (Aricept) On Behavioral And Psychological Symptoms In Patients With Severe Alzheimer's Disease [NCT00711204] | Phase 4 | 0 participants (Actual) | Interventional | 2008-01-31 | Withdrawn(stopped due to No patients were enrolled in the study.) | ||
| Study AZ3110866, a Fixed Dose Study of SB-742457 Versus Placebo When Added to Existing Donepezil Treatment in Subjects With Mild-to-moderate Alzheimer's Disease [NCT00710684] | Phase 2 | 682 participants (Actual) | Interventional | 2008-07-01 | Completed | ||
| Donepezil Treatment for Sleep Apnea Patients: A Double Blind Placebo-Controlled Study [NCT00912457] | Phase 4 | 60 participants (Anticipated) | Interventional | 2007-03-31 | Recruiting | ||
| An Investigation of the Relationship Between Donepezil Enhanced REM Sleep, Sleep Architecture and Behavior in the Prepubertal Child With Autism [NCT00695136] | Phase 1/Phase 2 | 17 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Three Way Interaction Between Gabapentin, Duloxetine, and Donepezil in Patients With Diabetic Neuropathy [NCT00619983] | Phase 4 | 22 participants (Actual) | Interventional | 2008-02-29 | Terminated(stopped due to Study terminated due to low enrollment) | ||
| A 4-Period, Placebo-Controlled, Crossover Study to Evaluate the Utility and Feasibility of BOLD fMRI and Cerebral Blood Flow Measurements as Biomarkers for Cognition Enhancing Drugs (Donepezil and MK3134) [NCT00887601] | Phase 1 | 32 participants (Actual) | Interventional | 2007-08-31 | Completed | ||
| Donepezil and Memantine in Moderate to Severe Alzheimer's Disease [NCT00866060] | Phase 4 | 800 participants (Anticipated) | Interventional | 2008-02-29 | Recruiting | ||
| Donepezil to Promote Functional Recovery Post-stroke [NCT00868010] | Phase 3 | 200 participants (Anticipated) | Interventional | 2009-03-31 | Recruiting | ||
| A Methodology Study To Evaluate Cerebrospinal Fluid Acetylcholine Following A Single Dose Administration Of Donepezil In Healthy Subjects [NCT00987220] | 12 participants (Actual) | Observational | 2009-10-31 | Completed | |||
| A Phase 2, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study to Evaluate the Efficacy and Safety of PRX-03140 as Monotherapy in Subjects With Alzheimer's Disease [NCT00693004] | Phase 2 | 236 participants (Anticipated) | Interventional | 2008-05-31 | Terminated | ||
| A Randomized, Double-Blind, Placebo-Controlled, Ascending-Dose Phase 1b Safety Study of Three Different Doses of an Alpha-7 Nicotinic Acetylcholine Receptor Agonist (EVP-6124) or Placebo in Patients With Mild to Moderate Probable Alzheimer's Disease [NCT00766363] | Phase 1 | 49 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| Effect of Donepezil on Speech Recognition in Cochlear Implant Users [NCT05438264] | Early Phase 1 | 50 participants (Anticipated) | Interventional | 2023-03-10 | Recruiting | ||
| Mayo Acute Stroke Trial for Enhancing Recovery [NCT00805792] | Phase 2 | 33 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
| Population Pharmacokinetic and Pharmacodynamic Modeling of Gabapentin in Neuropathic Pain - Effect of Adjuvant Pharmacotherapy [NCT00967707] | Phase 2 | 30 participants (Anticipated) | Interventional | 2009-08-31 | Completed | ||
| A 10-Week, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Donepezil Hydrochloride (Aricept®) in the Treatment of the Cognitive Dysfunction Exhibited by Children With Down Syndrome [NCT00570128] | Phase 2 | 129 participants (Actual) | Interventional | 2007-11-16 | Completed | ||
| A Double-Blind, Placebo-Controlled, Balanced, 4-Way, Incomplete Block Design to Evaluate the Effects of a Single Administration of SAM-531 on Sleep Electroencephalogram (EEG) and Quantitative Wake EEG (qEEG) in Healthy Subjects [NCT00519298] | Phase 1 | 25 participants (Anticipated) | Interventional | 2007-10-31 | Completed | ||
| Double-blind Study of E2020 in Patients With Dementia With Lewy Bodies - Phase II [NCT00543855] | Phase 2 | 167 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| Effects of the Cholinesterase Inhibitor Donepezil on Organic and Functional Deficits Associated With Age-Related Decrease of Growth Hormone [NCT00533065] | 80 participants (Actual) | Interventional | 2007-09-30 | Completed | |||
| Efficacy of Donepezil in Normalizing Brain Activation Patterns in People Genetically at Risk for Alzheimer's Disease [NCT00408525] | Phase 1 | 41 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
| A Single-centre, Randomised, Double-blind, Placebo-controlled, Four-period Cross-over Study to Evaluate the Scopolamine Cognition Model in Healthy Male Subjects Using AZD1446 and Donepezil Versus Placebo [NCT01044342] | Phase 1 | 20 participants (Anticipated) | Interventional | 2009-12-31 | Completed | ||
| A Study of the Effect of Concomitant Administration of BMS-708163 on the Pharmacokinetics of Donepezil in Healthy Subjects [NCT01042314] | Phase 1 | 18 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| An Open-Label Trial Of Donepezil in Vascular and Mixed Dementia [NCT00174382] | Phase 3 | 149 participants (Actual) | Interventional | 2005-06-30 | Terminated(stopped due to See Detailed Description) | ||
| Donepezil for Cancer Patients With Sedation Related to Opioid Treatment: A Double-blind Placebo Controlled Randomized Study [NCT00352664] | Phase 3 | 27 participants (Actual) | Interventional | 2003-11-30 | Terminated(stopped due to Low patient accrual) | ||
| Pharmacokinetics Study of Donepezil HCl in Subjects Receiving Haemodialysis. [NCT01063556] | Phase 4 | 6 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
| A 12-Week, Multicenter, Open-Label Study to Evaluate the Effectiveness and Safety of Donepezil Hydrochloride (Aricept) in Hispanic Patients With Mild to Moderate Alzheimer's Disease [NCT00230568] | Phase 4 | 100 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
| Comparative Assessment of Clinical Efficacy of Donepezil Between the Naive Group and the Switching Group [NCT01023425] | 72 participants (Actual) | Interventional | 2008-02-29 | Completed | |||
| Recovery From Amblyopia With Cholinesterase Inhibitors [NCT01584076] | Phase 1 | 18 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
| A Double-Blind, Placebo- and Positive-Controlled, Randomized, Partial 6-way Crossover Study to Investigate the Pharmacodynamics and Pharmacokinetics of CEP-26401 (5, 25, and 125 μg) Following Single-Dose Administration to Healthy Subjects [NCT01903824] | Phase 1 | 40 participants (Actual) | Interventional | 2013-08-31 | Completed | ||
| Comparison of Therapeutic Strategies With Cholinesterase Inhibitors: Stop or Still (SOS) Trial [NCT03454646] | Phase 4 | 1,205 participants (Anticipated) | Interventional | 2024-06-01 | Not yet recruiting | ||
| Lewy Body Spectrum Disorders: Investigating Neuropsychiatric Benefit and Adverse Effects in Response to Cholinesterase Inhibitors Using Genetics and Brain SPECT [NCT01944436] | 57 participants (Actual) | Observational | 2006-09-30 | Completed | |||
| [11C]Donepezil PET For Imaging The Autonomous Nervous System In Parkinsons Disease [NCT02012595] | 24 participants (Actual) | Observational | 2013-10-31 | Completed | |||
| Estrogen Modulation Effects on Cholinergic Function in Normal Post-Menopausal Women and Patients With Alzheimer's Disease [NCT00006399] | Phase 2 | 45 participants | Interventional | 1999-09-30 | Completed | ||
| An Exploratory Trial of Donepezil and Vitamin E to Prevent Cognitive Dysfunction in Patients With Small Cell Lung Cancer (SCLC) After Cancer Treatment Which Includes Prophylatic Cranial Irradiation (PCI) [NCT00006349] | Phase 3 | 9 participants (Actual) | Interventional | 2001-02-28 | Completed | ||
| Effects of Combining Donepezil, Intensive Language Rehabilitation and Transcranial Direct Current Stimulation on Language Recovery and Brain Reorganization in Chronic Post-stroke Aphasia [NCT04134416] | Phase 3 | 20 participants (Actual) | Interventional | 2019-01-08 | Completed | ||
| A Phase 1, Open-Label, 3-Period, Randomized, Crossover Pharmacokinetic Study to Evaluate the Steady-State Pharmacokinetics of 5 mg and 10 mg Corplex™ Donepezil Transdermal Delivery Systems Compared to 10 mg Oral Administration of Aricept® in Healthy Volun [NCT04617782] | Phase 1 | 60 participants (Actual) | Interventional | 2020-12-08 | Completed | ||
| Double-Blind, Parallel-Group Comparison of 23 mg Donepezil Sustained Release (SR) to 10 mg Donepezil Immediate Release (IR) in Patients With Moderate to Severe Alzheimer's Disease [NCT00478205] | Phase 3 | 1,467 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| Adjunctive Donepezil Therapy and Genetic Risk Factors of Cognitive Dysfunction in Brain Tumor Survivors [NCT00594633] | Phase 1 | 25 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
| A Methodology Study To Evaluate The Acute Effects Of Donepezil On Regional Cerebral Perfusion And Cognition In Subjects With Amnestic MCI And Mild Alzheimer's Disease [NCT01082965] | 18 participants (Actual) | Interventional | 2010-07-31 | Terminated(stopped due to The study was terminated because of slow enrollment. The decision to terminate the trial was not based on any safety or efficacy concerns.) | |||
| A 10-Week, Double-Blind, Placebo-Controlled Study To Evaluate The Efficacy And Safety Of Donepezil Hydrochloride (Aricept) In The Treatment Of The Cognitive Dysfunction Exhibited By Children With Down Syndrome, Aged 6 To 10 [NCT00754013] | Phase 3 | 9 participants (Actual) | Interventional | 2008-09-30 | Terminated(stopped due to Sufficient evidence of efficacy not met.) | ||
| A Multicenter, Double-blind, Parallel-group, Placebo-controlled Study of the Effect on Cognitive Performance and Safety/Tolerability of SSR180711C for 4 Weeks, Using Donepezil as Calibrator, in Patients With Mild Alzheimer's Disease [NCT00602680] | Phase 2 | 1 participants (Actual) | Interventional | 2008-01-31 | Terminated(stopped due to Insufficient expected benefit risk) | ||
| DL-3-n-butylphthalide Treatment in Patients With Mild to Moderate Alzheimer's Disease Already Receiving Donepezil : A Multi Center, Prospective Cohort Stud [NCT02711683] | 92 participants (Actual) | Observational | 2016-03-31 | Completed | |||
| A Randomized Clinical Trial To Evaluate the Single Dose Acute Effects of MK-0249 and Donepezil On Cognitive Function In Adult Patients With Alzheimer's Disease [NCT00874939] | Phase 1 | 4 participants (Actual) | Interventional | 2009-04-06 | Terminated | ||
| Randomized, Placebo-Controlled Study in Elderly Alzheimer's Patients on Established/Well Tolerated Dose of Aricept to Assess Skin Tolerability, Irritation, Adhesion With 3 Consecutive 7-Day Applications of 350 mg Donepezil Transdermal Patch [NCT00916383] | Phase 2 | 49 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| Ecological Perspective On The Efficacy And Tolerability Of Donepezil In A Routine Clinical Practice: A Patient Centered Observational Study [NCT00843115] | 370 participants (Actual) | Observational | 2007-02-28 | Terminated(stopped due to See Detailed Description.) | |||
| A Study to Investigate the Pharmacokinetic Drug-drug Interaction Following Oral Administration of BI 409306 and Donepezil in Healthy Male and Female Subjects [NCT02635750] | Phase 1 | 32 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
| Non-Interventional Study With Aricept® Evess In Patients Diagnosed With Mild And Moderate Alzheimer's Disease Or Vascular Dementia [NCT00889603] | 370 participants (Actual) | Observational | 2009-05-31 | Completed | |||
| A 24-weeks, Multi-center, Randomized, Double-blind, Placebo Controlled Study to Evaluate the Efficacy and Safety of Donepezil Hydrochloride in Chinese Subjects With Severe Alzheimer's Disease [NCT01404169] | Phase 3 | 260 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| An Open Label, Randomized, 2-Period, 2-Treatment, Crossover, Single-Dose Bioequivalence Study of Donepezil Hydrochloride Tablets 10mg [Test Formulation, Torrent Pharmaceutical Limited., India] Versus Aricept® (Donepezil Hydrochloride) Tablets 10mg [Refere [NCT01419340] | Phase 1 | 0 participants | Interventional | Completed | |||
| An Open Label, Randomized, 2-Period, 2-Treatment, Crossover, Single-Dose Bioequivalence Study of Donepezil Hydrochloride Tablets 10mg [Test Formulation, Torrent Pharmaceutical Limited., India] Versus Aricept® (Donepezil Hydrochloride) Tablets 10mg [Refere [NCT01419366] | Phase 1 | 0 participants | Interventional | Completed | |||
| [NCT00165659] | Phase 2 | 0 participants | Interventional | 2002-11-30 | Completed | ||
| A 24-Week, Multi-Center, Randomized, Double-Blind, Placebo-Controlled Evaluation of the Efficacy, Safety and Tolerability of Donepezil Hydrochloride (E2020) in Patients With Dementia Associated With Cerebrovascular Disease [NCT00165737] | Phase 3 | 974 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
| [NCT00165815] | Phase 3 | 0 participants | Interventional | 2002-08-31 | Completed | ||
| Randomized, Open-Label, 2-Way Crossover, Bioequivalence Study of Donepezil 10 mg Tablet and Aricept® (Reference) Following a 10 mg Dose in Healthy Subjects Under Fasting Conditions [NCT01439230] | Phase 1 | 36 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| Correlation Between Regional Brain Volume and Response to Donepezil Treatment in AD Patients [NCT00165750] | Phase 4 | 40 participants (Actual) | Interventional | 2005-03-31 | Terminated(stopped due to Lack of patients to enroll.) | ||
| [NCT00220896] | Phase 4 | 37 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
| A Multicenter, Randomized, Open-label, Prospective Study to Estimate the add-on Effects of Memantine as Ebixa Oral Pump on Language in Moderate to Severe Alzheimer's Disease Patients Already Receiving Donepezil. [NCT01849042] | Phase 4 | 188 participants (Anticipated) | Interventional | 2013-01-31 | Recruiting | ||
| [NCT01860625] | Phase 1 | 36 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
| Corticolimbic Degeneration and Treatment of Dementia [NCT00768261] | Phase 4 | 39 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
| Single Dose Crossover Comparative Bioavailability Study of Donepezil 23 mg Tablets in Healthy Male and Female Volunteers / Fed State [NCT01923259] | Phase 1 | 94 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| A 3-Month, Randomized, Double-Blind, Placebo-Controlled, Multicenter, Safety, Tolerability, and Efficacy Study Of 3 Doses Of Lecozotan (SRA-333) SR In Outpatients With Mild To Moderate Alzheimer's Disease With Donepezil As Active Control. [NCT00151398] | Phase 2 | 229 participants (Actual) | Interventional | 2005-10-06 | Completed | ||
| A Randomized, Double Blind, Placebo Controlled Study to Investigate the Effect of Donepezil and Gabapentin Combination on an Experimental Pain Model in Healthy Subjects [NCT01485185] | Phase 1 | 48 participants (Actual) | Interventional | 2011-10-11 | Completed | ||
| Donepezil Adjunctive Treatment for Cognitive Impairment in Schizophrenia [NCT01490567] | Phase 4 | 80 participants (Anticipated) | Interventional | 2011-06-30 | Recruiting | ||
| [NCT01495195] | Phase 2 | 12 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| Combining a Caregiver Intervention With Aricept Treatment for Mild to Moderate Alzheimer's Disease [NCT00467766] | 300 participants (Actual) | Interventional | 1999-07-31 | Completed | |||
| The Effect of Anticholinesterase Drugs on Sleep in Alzheimer's Disease Patients [NCT00480870] | Phase 4 | 65 participants (Actual) | Interventional | 1999-04-30 | Completed | ||
| A Multi-centre, Double-blind, Double-dummy, Placebo Controlled Parallel Group Randomized Phase IIb Proof of Concept Study With 3 Oral Dose Groups of AZD3480 or Donepezil During 12 Weeks Treatment in Patients With Alzheimer's Disease [NCT00501111] | Phase 2 | 659 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| [NCT00530478] | 0 participants | Interventional | Recruiting | ||||
| Functional Neuroimaging (fMRI) Biomarker of Allosteric Nicotinic Receptor Modulation in Mild Alzheimer's Disease Patients: A Razadyne vs. Aricept Dose Escalation Trial [NCT00369603] | Phase 4 | 4 participants (Actual) | Interventional | 2006-10-31 | Terminated(stopped due to Reduced access to AchEI medication-naive mild AD patients.) | ||
| A Relative Bioavailability Study of 10 mg Donepezil Hydrochloride Orally Disintegrating Tablets Under Fasting Conditions. [NCT01260922] | Phase 1 | 26 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
| Donepezil Attenuate Postoperative Cognitive Dysfunction in Aged Patients- A Multi-center, Case Control, Randomized Clinical Trail [NCT02927522] | Phase 3 | 550 participants (Anticipated) | Interventional | 2018-09-01 | Recruiting | ||
| Clinical Study on Improving the Cognitive Function of Patients With Mild to Moderate Alzheimer's Disease by Using Ginkgo Biloba Dispersible Tablets [NCT03090516] | Phase 2/Phase 3 | 240 participants (Anticipated) | Interventional | 2016-08-10 | Recruiting | ||
| A Randomized, Double-blind, Placebo-controlled, Single-dose, 6-Period Crossover Study to Evaluate the Effects of BPN14770 on Scopolamine-induced Cognitive Impairment in Healthy Volunteers [NCT03030105] | Phase 1 | 38 participants (Actual) | Interventional | 2017-01-31 | Completed | ||
| A Randomised, Double-blind, Double-dummy, Oral Donepezil Controlled Study on the Safety and Efficacy of Repeated Monthly Subcutaneous Injections of a Sustained-release Implant of ZT 1 in Patients With Moderate Alzheimer's Disease [NCT00423228] | 228 participants (Actual) | Interventional | 2007-02-28 | Completed | |||
| A Study to Evaluate A Study to Evaluate the Relative Bioavailability of Donepezil Hydrochloride 10 mg Tablets (OHM Laboratories, Inc., USA) Compared to ARICEPT® (Donepezil Hydrochloride)10 mg Tablets (Eisai Inc.) in Healthy Volunteers Under Non-Fasted Con [NCT01276080] | Phase 1 | 36 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| A Feasibility Study of Donepezil in Female Breast Cancer Survivors With Self-Reported Cognitive Dysfunction Following Chemotherapy [NCT01466270] | Phase 2 | 62 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
| Brain Imaging and Mental Disorders of Aging Intervention [NCT00267163] | Phase 4 | 64 participants (Actual) | Interventional | 2000-09-30 | Completed | ||
| A One-Year, Multicenter, Randomized, Double-Blind, Placebo-Controlled Evaluation of the Efficacy and Safety of Donepezil Hydrochloride in Subjects With Mild Cognitive Impairment (MCI) [NCT00293176] | Phase 4 | 821 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
| Randomized, Open-Label, 2-Way Crossover, Bioequivalence Study of Donepezil (Test) 10 mg Tablet and Aricept® (Reference) Following a 10 mg Dose in Healthy Subjects Under Fed Conditions [NCT01439243] | Phase 1 | 26 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| Monitoring Drug Efficacy Through Multi-omics Research Initiative in Alzheimer's Disease [NCT05801380] | 60 participants (Anticipated) | Observational | 2022-02-14 | Recruiting | |||
| A Double-Blind, Crossover Trial of Aricept® in Memory-Impaired Patients With Multiple Sclerosis: A Phase IV Demonstration of Functional MRI (fMRI) as a Surrogate Marker of Brain Activity Associated With Improvement in Memory Function [NCT00315367] | Phase 4 | 26 participants (Anticipated) | Interventional | 2004-09-30 | Completed | ||
| Evaluation of the Efficacy of Donepezil in the Treatment of Oxaliplatin-induced Peripheral Neuropathy: Proof of Concept Study [NCT05254639] | Phase 2 | 80 participants (Anticipated) | Interventional | 2022-06-02 | Recruiting | ||
| A 24 Week, Multicenter, Randomized, Double-Blind, Placebo-Controlled Evaluation of the Safety and Efficacy of Donepezil Hydrochloride (E2020) in Patients With Severe Alzheimer's Disease Followed by a 12 Week Open-Label Extension Period [NCT00096473] | Phase 3 | 229 participants (Actual) | Interventional | 2001-01-31 | Completed | ||
| Donepezil Double Blind Trial for ECT Memory Disfunction [NCT00465283] | Phase 4 | 40 participants (Anticipated) | Interventional | 2007-05-31 | Recruiting | ||
| A Randomized Double-Blind, Parallel, Placebo-Controlled Trial to Examine the Efficacy of Oral Donepezil (5 mg QD for 6 Weeks) After Single Dose and Steady State Therapy (2 Weeks and 6 Weeks) in Subjects With Mild Cognitive Impairment [NCT00483028] | 38 participants | Interventional | 2004-06-30 | Completed | |||
| Study of the Distractibility Syndrome in Patients With Progressive Supranuclear Palsy [NCT00139373] | Phase 2 | 16 participants (Anticipated) | Interventional | Recruiting | |||
| A Pilot Study of Donepezil Hydrochloride in Pediatric Brain Tumor Survivors After Cranial Irradiation [NCT00452868] | Early Phase 1 | 14 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| An Open-Label Trial of Donepezil in Fragile X Syndrome [NCT00220584] | Phase 1 | 10 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
| Effect of a 15-day Donepezil Treatment on Biomarkers of AD in Healthy Volunteers [NCT01487395] | Phase 1 | 30 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
| A Study to Evaluate the Relative Bioavailability of Donepezil Hydrochloride 10 mg Tablets (OHM Laboratories, Inc., USA) Compared to ARICEPT® (Donepezil Hydrochloride) 10 mg Tablets (Eisai Inc.) in Healthy Volunteers Under Fasted Conditions. [NCT01276067] | Phase 1 | 32 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| Phase 1 Study of Aricept Plus a Behavioral Strategy to Improve Functional Tasks in Vascular Dementia [NCT00457769] | Phase 1 | 18 participants (Anticipated) | Interventional | 2007-05-31 | Active, not recruiting | ||
| Memantine Versus Donepezil in Mild to Moderate Alzheimer's Disease. A Randomized Trial With Magnetic Resonance Spectroscopy. [NCT00505167] | Phase 4 | 64 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| Probable Alzheimer Type Dementia Compare INM-176 1200~1600mg/Day With Donepezil 5~10mg/Day of Safety and Efficacy to Randomization, Multicenter, Double-blind, Double-dummy, Parallel Phase III Clinical Study [NCT01245530] | Phase 3 | 280 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| A Randomised-controlled Trial of Donepezil for Motor Recovery in Acute Stroke [NCT01442766] | Phase 1/Phase 2 | 10 participants (Actual) | Interventional | 2011-11-30 | Terminated(stopped due to No financial support) | ||
| A Randomized, Double-Blind, Placebo-Controlled Trial of Vitamin E and Donepezil HCL (Aricept) to Delay Clinical Progression From Mild Cognitive Impairment (MCI) to Alzheimer's Disease (AD) [NCT00000173] | Phase 3 | 0 participants | Interventional | 1999-03-31 | Completed | ||
| Donepezil for Dementia in Parkinson's Disease: A Randomized, Double Blinded Placebo Controlled Crossover Trial [NCT00030979] | Phase 4 | 28 participants | Interventional | 2002-02-28 | Completed | ||
| Prevention of Cognitive Decline in Alzheimer's Disease by Ingested Interferon Alpha [NCT00031018] | Phase 2 | 0 participants | Interventional | Active, not recruiting | |||
| Cognitive Enhancers Explored With PET Imaging [NCT00042172] | Phase 4 | 40 participants | Interventional | 2002-06-30 | Completed | ||
| A Randomised Placebo Controlled Trial of a Cholinesterase Inhibitor in the Management of Agitation in Dementia That is Unresponsive to a Psychological Intervention [NCT00142324] | Phase 4 | 190 participants | Interventional | 2003-11-30 | Active, not recruiting | ||
| Double-Blind, Positive Comparator, Randomized, Parallel Study of Efficacy, Safety, and Tolerability of AZD3480 (TC-1734-226) as Monotherapy in Patients With Mild to Moderate Dementia of the Alzheimer's Type [NCT01466088] | Phase 2 | 386 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| A Phase 1 Study of E2022 Tape Formulation for Different Application Sites and Intervals [NCT01843556] | Phase 1 | 48 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
| Verbal Memory ERPs as Indices of Treatment Response in Alzheimer Disease [NCT00018278] | Phase 4 | 0 participants | Interventional | 1998-10-31 | Completed | ||
| A Based on PEEG and PET Study of Anxiolytic Treatment to Improve Cognitive Function in Patients With Alzheimer Disease [NCT03151382] | Phase 4 | 30 participants (Anticipated) | Interventional | 2017-05-20 | Not yet recruiting | ||
| Olfactory Deficits and Donepezil Treatment in Cognitively Impaired Elderly [NCT01951118] | Phase 4 | 121 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| Phase 1 Pharmacokinetic (PK) Study to Evaluate Once-weekly Corplex™ Donepezil Transdermal Delivery System Compared to Daily Oral Administration of Aricept® in Healthy Adult Subjects [NCT02968719] | Phase 1 | 107 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
| Donepezil and EGb761 in Improving Neurocognitive Function in Patients Who Have Previously Undergone Radiation Therapy for Primary Brain Tumor or Brain Metastases [NCT00070161] | Phase 2 | 68 participants (Actual) | Interventional | 2001-07-01 | Completed | ||
| PHARMACOLOGICAL TREATMENT OF COGNITIVE DEFICITS IN SCHIZOPHRENIC PATIENTS: The Effects of Central Cholinergic Augmentation on Cognitive Deficits and Psychopathology [NCT00206947] | Phase 2 | 50 participants (Anticipated) | Interventional | 2002-12-31 | Terminated(stopped due to No more funding) | ||
| Memory and Mental Health in Aging [NCT00043589] | 200 participants | Interventional | 2002-06-30 | Completed | |||
| An Open Label Study on the Efficacy and Safety of Donepezil Hydrochloride (Aricept) in Vascular Dementia [NCT00165763] | Phase 4 | 36 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
| Preventing Post-Operative Cognitive Decline [NCT00182845] | Phase 4 | 30 participants | Interventional | 2005-02-28 | Completed | ||
| Preventing Delirium in Hospitalized Elderly [NCT00182884] | Phase 4 | 30 participants | Interventional | 2004-07-31 | Completed | ||
| Open-Label, Multicentre, One Year Extension of the Evaluation of the Safety of Donepezil Hcl in Patients With Dementia Associated With Cerebrovascular Disease [NCT00188812] | Phase 3 | 0 participants | Interventional | 2004-05-31 | Completed | ||
| Donepezil as Add-On Treatment of Psychotic Symptoms in Patients With Dementia of the Alzheimer's Type [NCT00190021] | Phase 3 | 80 participants (Anticipated) | Interventional | Not yet recruiting | |||
| Treatment With Donepezil of Chronic Aphasia and Sensorimotor Deficits Associated to Cerebrovascular Accidents: a Double-Blind,Placebo-Controlled, Randomized Parallel Trial. [NCT00196690] | Phase 4 | 30 participants | Interventional | 2003-02-28 | Completed | ||
| Interventions to Improve Memory in Patients With Multiple Sclerosis [NCT00062972] | Phase 3 | 0 participants (Actual) | Interventional | 1999-09-30 | Withdrawn(stopped due to Study terminated/withdrawn) | ||
| Donepezil for Residual Symptoms in CPAP Treated Obstructive Sleepapnea Patients: A Controlled Study [NCT03299257] | Phase 4 | 36 participants (Anticipated) | Interventional | 2018-07-06 | Not yet recruiting | ||
| Donepezil Effects on Cocaine Craving and Pharmacokinetics [NCT00467389] | Phase 2 | 12 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
| Improving Walking Automaticity in Parkinson's Disease: Levodopa or Donepezil [NCT03599726] | Early Phase 1 | 20 participants (Actual) | Interventional | 2018-07-30 | Completed | ||
| A Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study of Donepezil Hydrochloride (E2020) in Patients With Dementia Associated With Cerebrovascular Disease [NCT02660983] | Phase 4 | 302 participants (Actual) | Interventional | 2013-08-05 | Completed | ||
| A Single Center Study To Examine Neural Correlates Of Cognition In Subjects With Mild Alzheimer's Disease After Three Months Of Open Label Donepezil HCl (Aricept® ) Treatment [NCT00477659] | Phase 4 | 14 participants (Actual) | Interventional | 2007-07-23 | Completed | ||
| A Multicenter, Randomized, Double-blind, Parallel-group, Placebo-controlled Study of E2020 in Patients With Dementia With Lewy Bodies (DLB), Followed by a Long-term Extension Phase [NCT01278407] | Phase 3 | 142 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| Olfactory Deficits in Mild Cognitive Impairment as a Predictor of Improved Cognition on Donepezil [NCT01845636] | Phase 4 | 41 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
| "[11C]Donepezil PET for Imaging the Parasympathetic Nervous System in Healthy Adults" [NCT01877538] | 7 participants (Actual) | Observational | 2013-05-31 | Completed | |||
| A Randomized Controlled Trial of Donepezil for REM Enhancement and Behavioral Change in Autism [NCT01887132] | Phase 2 | 5 participants (Actual) | Interventional | 2013-06-30 | Terminated | ||
| A Phase 2a Multicenter, Randomized, Double-Blind, Parallel Group, 26-Week, Placebo-Controlled Study of SUVN-502 in Subjects With Moderate Alzheimer's Disease Currently Treated With Donepezil Hydrochloride and Memantine Hydrochloride [NCT02580305] | Phase 2 | 564 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
| A Double-Blind, Randomised, Placebo-Controlled, Parallel Group Study to Investigate the Effects of SB-742457, Donepezil and Placebo on Cognition in Subjects With Mild to Moderate Alzheimer's Disease [NCT00348192] | Phase 2 | 200 participants | Interventional | 2006-05-31 | Completed | ||
| Open Label, Balanced, Randomized, Two-treatment, Two-period, Two Sequence, Single Dose, Crossover, Oral Bioequivalence Study of Donepezil Hydrochloride Tablets 10mg With ARICEPT® (Containing Donepezil Hydrochloride) Tablets 10 mg in Healthy, Adult, Human [NCT01504503] | Phase 1 | 26 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| Open Label, Balanced, Randomized, Two-treatment, Two-period, Two Sequence, Single Dose, Crossover, Oral Bioequivalence Study of Donepezil Hydrochloride Tablets 10mg With ARICEPT® (Containing Donepezil Hydrochloride) Tablets 10mg in Healthy, Adult, Human S [NCT01504516] | Phase 1 | 25 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| Multicenter, Randomized, Double-blinded, Placebo-controlled Clinical Trial of Donepezil for the Treatment of Mild Cognitive Impairment in Parkinson's Disease [NCT05709301] | Phase 2 | 120 participants (Anticipated) | Interventional | 2023-10-01 | Not yet recruiting | ||
| A Bioequivalence Study of Film-coated Tablet and Dry Syrup 1% Form for E2020 in Healthy Japanese Adult Males [NCT01506739] | Phase 1 | 12 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
| A Bioequivalence Study Comparing Improved Versus Current Orally Disintegrating E2020 10 mg Tablet in Healthy Japanese Adult Males [NCT01506752] | Phase 1 | 20 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
| Treatment of Delirium in the Elderly With Donepezil: a Double-blind, Randomized, Placebo-controlled Clinical Trial [NCT01633593] | Phase 4 | 19 participants (Actual) | Interventional | 2012-08-31 | Terminated(stopped due to Difficulty in recruiting subjects for the trial.) | ||
| Donepezil Effect on Visual Attention and Perceptual Training in Healthy Young Adults [NCT01738295] | 20 participants (Actual) | Interventional | 2013-01-31 | Completed | |||
| Comparison of Cerebrolysin and Donepezil: A Randomized, Double-blind, Controlled Trial on Efficacy and Safety in Patients With Mild to Moderate Alzheimer's Disease [NCT01822951] | Phase 4 | 0 participants (Actual) | Interventional | Withdrawn | |||
| Comparative Effectiveness Research Trial of Alzheimer's Disease Drugs [NCT01362686] | 200 participants (Actual) | Interventional | 2011-04-30 | Terminated(stopped due to Low study accrual caused the study to be ended early.) | |||
| Pilot Combination Treatment Trial of Mild Cognitive Impairment With Depression [NCT01658228] | Phase 4 | 86 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| Memory and Mental Health in Aging: Psychopharmacological Augmentation of Memory Training in Older Adults [NCT02988908] | Phase 4 | 198 participants (Actual) | Interventional | 2000-04-30 | Completed | ||
| The Combination of Donepezil and Cognitive Training for Treating Alcohol Use Disorder [NCT05042102] | Phase 2 | 160 participants (Anticipated) | Interventional | 2022-08-08 | Recruiting | ||
| Effects of 15-day Donepezil and Memantine on Cognitive Functions After a 24 Hours Sleep Deprivation Challenge in Healthy Volunteers: a Double-blind, Placebo-controlled, Randomised, Cross-over Study, With Modafinil as Positive Control [NCT01461174] | Phase 1 | 36 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
| A Phase II, Dose Titration Study of CPC-201 in Patients With Dementia of Alzheimer's Type [NCT02549196] | Phase 2 | 28 participants (Actual) | Interventional | 2015-10-07 | Completed | ||
| Technical R&D and Demonstration of Intelligent Medical Care in Alzheimer's Disease's Management [NCT05641480] | 150 participants (Anticipated) | Interventional | 2022-06-03 | Recruiting | |||
| The Effect of Acetylcholinesterase Inhibitors on Smoking Behavior [NCT01250977] | Phase 2 | 30 participants (Actual) | Interventional | 2011-01-11 | Completed | ||
| Randomized, Multicenter, Double-blind, Double-dummy, Parallel-Group Study With an Open-label Extension Phase to Compare the Efficacy and Safety of Donepezil Hydrochloride 23 mg Treatment With Continuation of Donepezil Hydrochloride 10 mg Treatment in Japa [NCT01539031] | Phase 3 | 351 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| A Multicenter, Randomized, Double-blind, Placebo-controlled, Phase IIb, Clinical Study to Evaluate the Safety and Efficacy of DHP1401 in Patients With Mild-moderate Alzheimer's Disease Treated With Donepezil(DRAMA) [NCT03055741] | Phase 2 | 180 participants (Actual) | Interventional | 2016-12-28 | Completed | ||
| Immunohistochemical Study of Peripheral Blood Mononuclear Cells in Sporadic Alzheimer's Disease and Dementia With Lewy Body [NCT05518409] | 100 participants (Anticipated) | Interventional | 2022-04-01 | Recruiting | |||
| A Study to Characterize LY3314814 Pharmacokinetics as a Function of Dosing Duration and to Determine the Effect of LY3314814 on the Pharmacokinetics of CYP3A Substrates in Healthy Subjects [NCT02406261] | Phase 1 | 82 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
| A 28-Week Open Label Extension Study Evaluating Safety and Tolerability of Donepezil Hydrochloride in Subjects With Mild Cognitive Impairment [NCT00934375] | Phase 4 | 145 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| Single Dose Crossover Comparative Bioavailability Study of Donepezil 23 mg Tablets in Healthy Male and Female Volunteers / Fasting State [NCT01923558] | Phase 1 | 76 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| Donepezil/ Galantamine in the Treatment of Post-stroke Cognitively Impaired Rehabilitating Elderly [NCT00227994] | Phase 4 | 40 participants (Actual) | Interventional | 2003-04-30 | Completed | ||
| Effect of Acetylcholinesterase Inhibitors on the Gait of the Patients With Parkinson Disease Characterized by Postural Instability and Gait Disturbance [NCT03011476] | Phase 4 | 20 participants (Anticipated) | Interventional | 2017-04-11 | Recruiting | ||
| A Multi-centre, Double-blind, Parallel-group, Randomised Controlled Study to Investigate Efficacy, Safety and Tolerability of Orally Administered BI 409306 During a 12-week Treatment Period Compared to Placebo in Patients With Cognitive Impairment Due to [NCT02337907] | Phase 2 | 329 participants (Actual) | Interventional | 2015-01-21 | Completed | ||
| [NCT00004807] | 120 participants | Interventional | 1995-01-31 | Completed | |||
| The Impact of Arousal Threshold in Obstructive Sleep Apnea: Donepezil's Effects on the Arousal Threshold and on the Apnea Hypopnea Index [NCT02264353] | Phase 4 | 44 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
| The Effect of Donepezil on Perceptual Learning in Adult Amblyopia [NCT03109314] | Phase 4 | 20 participants (Actual) | Interventional | 2012-05-01 | Completed | ||
| A Randomized, Double-Blind, Placebo Controlled, 4-Period, Cross-Over Study to Evaluate the Effects of Single Oral Administrations of Roflumilast in Combination With Donepezil on Reversing Scopolamine (Hyoscine) Induced Deficits in Psychomotor and Cognitiv [NCT02051335] | Phase 1 | 27 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| A Clinical Study to Evaluate a Cognitive Platform to Support Development of Symptomatic Therapies in Participants at Risk for Alzheimer's Disease [NCT04730635] | Phase 1 | 44 participants (Actual) | Interventional | 2021-03-23 | Completed | ||
| Effects of Cholinergic Augmentation on Measures of Balance and Gait [NCT02206620] | Phase 2 | 49 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
| Effect of Acetylcholinesterase Inhibitors on Bone Metabolism and Fracture Risk Factors Among Older Adults With Mild to Moderate Alzheimer's Disease [NCT06041789] | Phase 2 | 45 participants (Anticipated) | Interventional | 2023-12-04 | Not yet recruiting | ||
| Phase III Study of Shenwu Capsule in Treating Amnestic Mild Cognitive Impairment [NCT01451749] | Phase 3 | 324 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
| "Efficacy of Chinese Traditional Medicine Smart Soup in Cognition and Behavior Regulation in Alzheimer's Disease" [NCT05538507] | Phase 2 | 180 participants (Anticipated) | Interventional | 2022-06-01 | Recruiting | ||
| A Post-Marketing Clinical Study of Aricept in Patients With Dementia With Lewy Bodies (DLB) [NCT02345213] | Phase 4 | 160 participants (Actual) | Interventional | 2015-03-01 | Completed | ||
| An Open-label, Randomized, Cross-over, Multiple Dose, Phase 1 Clinical Trial to Evaluate the Safety, Pharmacokinetics and Pharmacodynamics of DA-5207 Transdermal Delivery System in Healthy Adults [NCT04479865] | Phase 1 | 49 participants (Actual) | Interventional | 2020-07-28 | Active, not recruiting | ||
| Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567] | Phase 3 | 407 participants (Actual) | Interventional | 2015-01-31 | Terminated | ||
| A Phase II, Multicenter, Randomized, Double-Blind, Parallel-Group, Placebo-Controlled Study to Investigate the Efficacy and Safety of RO4602522 Added to Background Alzheimer's Disease Therapy in Patients With Moderate Severity Alzheimer's Disease [NCT01677754] | Phase 2 | 542 participants (Actual) | Interventional | 2012-10-24 | Completed | ||
| Randomized, Blinded, Sham-Controlled Trial of Acupuncture on the Progression of Mild Alzheimer's Disease [NCT05078944] | 240 participants (Anticipated) | Interventional | 2022-06-30 | Recruiting | |||
| Monitoring Anti-Dementia Drugs by Serum Levels: Importance of Serum Levels, Drug-monitoring, Side-effects, Clinical Efficacy and Compliance (Translation of Official Danish Title) [NCT04117178] | Phase 4 | 132 participants (Actual) | Interventional | 2020-02-04 | Completed | ||
| Effects of Donepezil HCL on Task-Activated fMRI Brain Activation in Healthy Older Adults at Genetic Risk for Alzheimer's Disease [NCT02087865] | Phase 4 | 89 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| A Randomized, Double-blind, Placebo Controlled, Crossover Study to Evaluate the Effect of Donepezil on Gait and Balance in Parkinson's Disease [NCT01521117] | Phase 4 | 21 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
| A Randomized, Double Blind, Parallel-Group Comparison Study Versus E2020 10mg Followed by an Open-label Extension Phase to Explore the Safety of E2020 SR 23 mg in Japanese Subjects With Severe Alzheimer's Type Dementia [NCT01276353] | Phase 2 | 45 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| Evaluation of the Contribution of Regular Cognitive Exercises to Treatment in Patients With Alzheimer's Disease Receiving Donepezil, Memantine or Donepezil/Memantine Combination Therapy: Open-Labeled, Randomized, Phase IV, Superiority Study [NCT03954613] | Phase 4 | 198 participants (Anticipated) | Interventional | 2020-10-15 | Recruiting | ||
| Supporting the Health of Adults Undergoing Orthopedic Surgery During the Recovery Period [NCT00586196] | Phase 2 | 16 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| Effect of Donepezil on Prevention of Postoperative Urinary Retention in Patients Undergoing Extensive Total Hysterectomy [NCT05540977] | Early Phase 1 | 108 participants (Anticipated) | Interventional | 2022-08-01 | Recruiting | ||
| Study AZ3110865, a Study Comparing SB-742457 or Donepezil Versus Placebo in Subjects With Mild-to-moderate Alzheimer's Disease [NCT00708552] | Phase 2 | 576 participants (Actual) | Interventional | 2008-07-04 | Completed | ||
| A Phase 3 Randomized Placebo Controlled Clinical Trial of Donepezil in Chemotherapy Exposed Breast Cancer Survivors With Cognitive Impairment [NCT02822573] | Phase 3 | 276 participants (Actual) | Interventional | 2017-05-30 | Completed | ||
| Donepezil Compared to Placebo in Patients With Chronic Neuropathic Pain [NCT01743976] | Phase 4 | 5 participants (Actual) | Interventional | 2012-12-31 | Terminated(stopped due to Failure to recruit subjects) | ||
| Can Donepezil Preserve Autobiographical Memory Post Electroconvulsive Therapy? A Randomized, Placebo-Controlled Trial [NCT02331771] | 12 participants (Actual) | Interventional | 2015-09-24 | Terminated(stopped due to Lack of sufficient enrollment) | |||
| Efficacy and Safety of Donepezil and Sodium Oligomannate in Patients With Mild to Moderate Alzheimer's Disease [NCT05114499] | 150 participants (Anticipated) | Observational | 2021-12-31 | Not yet recruiting | |||
| Safety and Efficacy of Donepezil HCl 23 mg in Patients With Moderate to Severe Alzheimer's Disease [NCT02097056] | Phase 4 | 171 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
| A Clinical Trial to Assess Cognitive Function by Repeated Computerized Testing in Patients With Mild Alzheimer's Disease Treated With Donepezil [NCT02064920] | Phase 2 | 36 participants (Actual) | Interventional | 2014-04-22 | Completed | ||
| Donepezil Use Versus Non-drug Approach in Treatment of Newly Diagnosed Alzheimer's Disease : a Multicentric, Randomized, Open Study : the CHOLINE-2 Study [NCT04661280] | Phase 3 | 240 participants (Anticipated) | Interventional | 2022-02-10 | Recruiting | ||
| Donepezil HCl: Treating Cognitive Deficits in Autism [NCT00047697] | Phase 2 | 34 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
| An Open-label, Randomized, Cross-over, Multiple Dose, Phase 1 Clinical Trial to Evaluate the Safety, Pharmacokinetics and Pharmacodynamics of DA-5207 Transdermal Delivery System in Healthy Adults [NCT05127746] | Phase 1 | 51 participants (Actual) | Interventional | 2021-11-25 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||