ache-in-3

AChE-IN-3 had inhibitory effect on AChE and stronger inhibitory effect on NO, with EC50 of 0.57 μM.

sEH/AChE-IN-3 (15) serves as a dual inhibitor targeting both soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE), demonstrating potent activity and the ability to cross the blood-brain barrier (BBB). It exhibits IC50 values of 0.4 nM for human sEH (hsEH), 1.94 nM for human AChE (hAChE), 615 nM for human butyrylcholinesterase (hBChE), 4.3 nM for mouse sEH (msEH), and 2.61 nM for mouse AChE (mAChE), indicating its efficacy across these enzymes.

ACHE-IN-38 is a potent Acetylcholinesterase inhibitor that can be used for the synthesis of compounds with anti-inflammatory, anti-tumor, and antibacterial activities.

AChE/Aβ-IN-3 (Compound AM5) is a dual inhibitor of AChE and Amyloid-β aggregation, with IC₅₀ values of 1.29 and 4.93 μM, respectively. This compound exhibits antioxidant properties, reducing ROS and normalizing their levels. It is applicable in the study of neurological disorders such as Alzheimer's disease.

AChE/BChE-IN-3 (BMC-1) is a dual inhibitor of AChE and BChE, with IC50 values of 6.08 μM for electric eel AChE (elAChE) and 0.383 μM for equine serum BChE (eqBChE), respectively [1].

AChE/BChE-IN-3 (BMC-1) hydrochloride is a dual inhibitor of AChE and BChE, with IC50 values of 0.383 μM against equine serum BChE (eqBChE) and 6.08 μM against electric eel AChE (elAChE) [1].

AChE/BuChE-IN-3 is a potent inhibitor of AChE (IC50: 0.65 μM) and BuChE (IC50: 5.77 μM) that crosses the blood-brain barrier and inhibits the aggregation of Aβ1-42, suitable for Alzheimer's disease research.

AChE/BChE/MAO-B-IN-3, an indan-1-one derivative, is a potent inhibitor of human monoamine oxidase B (MAO-B) with an IC50 of 0.0359 μM and also demonstrates significant inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 0.0473 μM and 0.0782 μM, respectively. Exhibiting notable antioxidant activity, AChE/BChE/MAO-B-IN-3 holds considerable promise for Alzheimer's disease (AD) research.

AChE/MAO-B-IN-3 is a dual inhibitor targeting both acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B), exhibiting inhibitory concentrations (IC50s) of 0.0257 μM and 0.0456 μM against human AChE and MAO-B, respectively. This compound holds potential for Alzheimer's disease research.

Dual AChE-MAO B-IN-3 (Compound C10) is a potent inhibitor of both AChE and MAO-B, with IC50 values of 0.58 μM and 0.41 μM, respectively. It targets the catalytic anionic site and peripheral anionic site of AChE, making it relevant for Alzheimer's disease (AD) research [1].

hAChE-IN-3 (compound 5c) serves as a potent inhibitor for AChE, BuChE, MAO-B, and BACE-1, with respective IC50 values of 0.44, 0.08, 5.15, and 0.38 μM, demonstrating its ability to cross the blood-brain barrier. This compound also exhibits antioxidant properties and metal chelation capabilities. Additionally, it targets peripheral anion sites, potentially modulating β-amyloid and ameliorating neurodegeneration linked to Alzheimer's disease, highlighting its research potential for this condition [1].

eeAChE-IN-3 (compound YS3g) is an orally bioavailable and potent inhibitor of EeAChE and IL-6, with IC50 values of 0.54 μM for EeAChE, 0.49 μM for RatAChE, 8.54 μM for RatBuChE, and 0.57 μM for IL-6. It can enhance learning and memory deficits in mice induced by STZ (streptozotocin) and shows potential for Alzheimer's disease (AD) research.

AChE-IN-39 (Compound 7c), with an IC50 value of 0.058 μM, is an acetylcholinesterase (AChE) inhibitor known for its DPPH scavenging activity and potential to ameliorate cognitive impairments in an aluminum chloride (AlCl3)-induced amnesia animal model, suggesting its usefulness in Alzheimer's disease research [1].

AChE-IN-31 (compound 1), a non-competitive acetylcholinesterase (AChE) inhibitor, exhibits potential for Alzheimer's disease research [1].

AChE-IN-30 is an acetylcholinesterase (AChE) inhibitor exhibiting neuroprotective effects with an inhibitory concentration (IC 50) of 4.4 μM. It prevents hydrogen peroxide (H 2 O 2)-induced apoptosis by inhibiting the accumulation of reactive oxygen species (ROS) within cells and is utilized in Alzheimer's disease research [1].

AChE-IN-34 (compound 5l) is a potent and selective AChE inhibitor with an IC50 of 3.98 µM, exhibiting negligible BChE inhibition. It demonstrates mixed-mode inhibition of AChE with a Ki of 0.044 µM using acetylthiocholine substrate concentrations ranging from 0.1-1 mM [1].

AChE-IN-35 (compound 5g) is an acetylcholinesterase inhibitor with an IC50 value of 5.88 μM [1].

AChE-IN-36 (compound A4) is an acetylcholinesterase inhibitor with an IC50 of 0.04 μM, affecting ROS levels and modulating NRF2 gene expression [1].

AChE-IN-37 (compound A2) is an acetylcholinesterase inhibitor with an IC50 of 0.23 µM, altering reactive oxygen species (ROS) levels and modulating the expression of nuclear factor erythroid 2-related factor 2 (NRF2) [1].

hBChE-IN-3 (compound 30) serves as both an activator of carbonic anhydrase (CA) and an inhibitor of cholinesterase (ChE), exhibiting IC50 values of 7.4 nM for AchE and 1.9 nM for BchE. This compound is utilized in the research of neurodegenerative and psychiatric disorders.

Acotiamide is an orally active, selective, and reversible acetylcholinesterase (AChE) inhibitor with an IC50 of 1.79 μM. It is a gastroprokinetic agent that enhances gastric contractility and accelerates delayed gastric emptying, with potential for research in functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory [1] [2] [3].

6,9-Dichloro-1,2,3,4-tetrahydroacridine is a synthetic intermediate in the synthesis of tacrine-based acetylcholinesterase (AChE) inhibitors.1It is also an intermediate in the synthesis of multifunctional tacrine hybrids that possess radical scavenging, amyloid-β aggregation inhibitory, and/or β-secretase 1 (BACE1) inhibitory activities in addition to their activity as AChE inhibitors.2,3 1.Recanatini, M., Cavalli, A., Belluti, F., et al.SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: Synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analoguesJ. Med. Chem.43(10)2007-2018(2000) 2.Digiacomo, M., Chen, Z., Wang, S., et al.Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of ADBioorg. Med. Chem. Lett.25(4)807-810(2015) 3.Li, S.Y., Jiang, N., Xie, S.S., et al.Design, synthesis and evaluation of novel tacrine-rhein hybrids as multifunctional agents for the treatment of Alzheimer's diseaseOrg. Biomol. Chem.12(5)801-814(2014)

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2 1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

Rivastigmine carbamate impurity (3-Nitrophenyl ethyl(methyl)carbamate) is a byproduct found in Rivastigmine, a potent and orally active cholinesterase (ChE) inhibitor that effectively inhibits butyrylcholinesterase (BChE) and acetylcholinesterase (AChE) with IC50 values of 0.037 μM and 4.15 μM, respectively.