bche

AChE BChE MAO-B-IN-1 is a reversible, non-time-dependent inhibitor of AChE, BChE, and MAO-B that crosses the blood-brain barrier, exhibiting inhibitory effects on hAChE, hBChE, and hMAO-B with IC50s of 7.31, 0.56, and 26.1 μM, respectively. [AChE BChE MAO-B-IN-1] had a neuroprotective effect and was not significantly cytotoxic.

BChE HDAC6-IN-2 is a selective and potent dual inhibitor of BChE and HDAC6 with neuroprotective and reactive oxygen species (ROS) scavenging activity. BChE HDAC6-IN-2 is a metal ion co-agonist that inhibits tau phosphorylation and can be used in the study of immune and neurological diseases.

BChE-IN-19 (Compound 7b), a para-substituted indone derivative, exhibits potent inhibitory activity against butyryl cholinesterase (BChE) with an IC50 value of 0.04 μM. It enhances cholinergic neurotransmission and has potential therapeutic application in Alzheimer's disease [1].

AChE BChE-IN-14 (compound 13), a benzylisoquinoline alkaloid extracted from Fissistigma polyanthum roots, demonstrates inhibitory effects on both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), coupled with antioxidant properties, and is pertinent to Alzheimer’s disease research [1].

AChE BChE-IN-9 (Compound 7a) is a potent, orally active inhibitor of AChE and BChE, with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. It also demonstrates effective antioxidant activity (IC50 = 57.35 μM), chelates iron, and modulates amyloid β 1-42 aggregation. Notably, AChE-IN-16 can cross the blood-brain barrier [1].

BChE-IN-4 is a highly potent inhibitor of the enzyme butyrylcholinesterase, capable of crossing the blood-brain barrier. It effectively reduces learning and memory impairments resulting from a deficiency in cholinergic activity in a mouse model. BChE-IN-4 holds promise for further investigation in the field of Alzheimer's disease research [1].

BChE-IN-3 is a selective, selective, time-dependent, pseudo-irreversible inhibitor of BChE butyrylcholinesterase (IC50: 56.9 nM).BChE-IN-3 exhibits borderline reversible (time-independent) inhibition of AChE acetylcholinesterase.

BChE-IN-15 is a compound characterized as a pseudo-irreversible, covalent inhibitor of butyrylcholinesterase (BChE), demonstrating potent activity with an inhibitory concentration (IC50) of 1.76 nM against human BChE (hBChE).

BChE-IN-6 (compound 12) is a highly effective inhibitor of BChE with a Ki value of 0.182 μM, and it exhibits significant chelating abilities towards Zn 2+. These characteristics make BChE-IN-6 a valuable tool for researchers in the field of Alzheimer's disease (AD) [1].

AChE BChE-IN-1 is a potent dual inhibitor of acetylcholinesterase and butyrylcholinesterase with blood-brain barrier permeability, exhibiting IC50 values of 1.06 nM for hAChE and 7.3 nM for hBChE, and showing antioxidant effects. AChE BChE-IN-1 can be used in Alzheimer's disease research.

BChE-IN-5 is a potent and selective inhibitor of BChE (IC50: 2.8 nM) with a higher inhibitory effect on hBChE than hAChE and potential applications in Alzheimer's disease research.

AChE BChE BACE-1-IN-2 (Compound 4o) is an orally active AChE, BACE-1, and BChE inhibitor with IC50 values of 0.069, 0.097, and 0.127 μM against hAChE, hBACE-1, and hBChE, respectively. It exhibits remarkable antioxidant potential, considerable binding capability towards PAS-AChE, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress with excellent brain permeation [1].

BChE-IN-21, a potent inhibitor of butyrylcholinesterase (BChE), exhibits an inhibition constant (IC50) of 0.14 ± 0.02 μM, indicating promise for research in Alzheimer's disease [1].

AChE BChE-IN-2 (Compound 13b) is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 0.96 ± 0.14 μM for AChE and 1.23 ± 0.23 μM for BChE.

BChE-IN-9 (Azepano-11-deoxo-glycyrrhetol) is a hybrid butyrylcholinesterase (BChE) inhibitor with a Ki of 0.21 μM.

BChE-IN-13 (Compound 17c) is an orally active, potent, and selective inhibitor of Butyrylcholinesterase (BChE), exhibiting IC50 values of 0.22 μM and 0.016 μM for eqBChE and hBChE, respectively. BChE-IN-13 enhances memory and cognitive impairments, making it valuable for Alzheimer's disease (AD) research [1].

BChE-IN-16 (compound 87) is a potent inhibitor of human butyrylcholinesterase (hBChE) with an inhibition concentration half-maximum (IC50) of 3.8 nM. It demonstrates low cytotoxicity, potential for central nervous system (CNS) permeability, and unique adaptability, making it a valuable tool for Alzheimer's disease (AD) research.

AChE BChE-IN-15 (Compound 6d) is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 20 nM for AChE and 220 nM for BChE. It targets the catalytic anionic site (CAS) and the peripheral anionic site (PAS) within the enzymes' active centers. AChE BChE-IN-15 is applicable in Alzheimer’s disease research [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 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 BChE MAO-B-IN-4, an indan-1-one derivative, is a potent inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase butyrylcholinesterase (AChE BChE). It strongly inhibits human MAO-B with an IC50 of 0.0393 μM and is highly effective against human AChE and BChE with IC50 values of 0.0458 μM and 0.075 μM, respectively. Additionally, this compound exhibits significant antioxidant properties and ability to prevent β-amyloid plaque aggregation, suggesting its potential in Alzheimer's disease (AD) research.

BChE-IN-11, a selective and non-competitive inhibitor of butyrylcholinesterase (BChE), demonstrates potent activity with an inhibitory concentration (IC50) of 2.1 μM. This compound is applicable in Alzheimer's disease (AD) research.

AChE BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM against Electrophorus electricus AChE (EeAChE) and 2.364 μM against equine BChE (eqBChE), respectively. AChE BChE-IN-8 demonstrates blood-brain barrier permeability and low cytotoxicity.

AChE BChE-IN-5 (BMC-16) is a dual inhibitor of AChE and BChE that can cross the BBB, with IC50 values of 266 nM for human AChE (hAChE) and 10.6 nM for human BChE (hBChE) [1].

BChE-IN-14 (compound 19c) is a selective inhibitor of butyrylcholinesterase (BChE) with IC50 values of 0.011 μM for hBChE and 0.23 μM for eqBChE, exhibiting primary cell safety and good blood-brain barrier permeability. It can restore cognitive impairment in vivo and is useful in Alzheimer's disease research [1].

BChE HDAC6-IN-1 is a dual BChE HDAC6 inhibitor exhibiting potent and selective inhibition with IC50 values of 4 nM for BChE and 8.9 nM for HDAC6. It demonstrates efficacy in alleviating cognitive deficits in an Aβ1–42-induced mouse model, indicating its potential utility in Alzheimer's disease research [1].

BChE-IN-17 (compound 6n) is a potent and selective inhibitor of butyrylcholinesterase (BChE), with half-maximal inhibitory concentrations (IC50s) of 10.5 nM for equine BChE (eqBChE) and 32.5 nM for human BChE (hBChE). It shows over 1000-fold greater selectivity for BChE compared to acetylcholinesterase (AChE), while exhibiting low neurotoxicity and moderate neuroprotective effects [1].

AChE BChE-IN-11 (compound 1), a natural product derived from artichoke leaves, is a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 70 μM and 71 μM, respectively. This compound is used in Alzheimer’s disease (AD) research [1].

BChE-IN-7 (compound 13) is a potent, selective, and reversible inhibitor of AChE and BChE, with an IC50 value of 0.06 μM for BChE. It can cross the blood-brain barrier and protect neuronal-like cells from toxic Aβ-species [1].

AChE BChE-IN-10 is a potent dual inhibitor of AChE and BChE with IC50 values of 0.176, and 0.47 μM, respectively. AChE BChE-IN-10 exhibits good blood brain barrier permeability. AChE BChE-IN-10 can inhibit Aβ-aggregation.

BChE-IN-2 (compound 22) is a highly effective inhibitor of BChE, with a Ki value of 0.099 μM, and represents a promising pyrimidine and pyridine derivative for investigating Alzheimer's disease (AD). [1]

AChE BChE-IN-13 (compound 5j) serves as a potent dual inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting half-maximal inhibitory concentrations (IC50) of 20.89 μM for AChE and 17.37 μM for BChE, and is applicable in research related to Alzheimer's disease (AD) [1].

BChE-IN-8 (compound 20) is an orally active butyrylcholinesterase (BChE) inhibitor that crosses the blood-brain barrier, targeting eqBChE (IC50: 0.15 nM) and hBChE (IC50: 45.2 nM). It is used in Alzheimer's disease (AD) research for its neuroprotective and cognitive improvement effects, affecting the cholinergic system, Aβ aggregation, and neuropeptide levels.

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 MAO-B-IN-2 is a potent inhibitor of the enzymes AChE, BChE, and MAO-B, with IC50 values of 48.2 nM, 83.9 nM, and 31.2 nM, respectively. It also exhibits significant antioxidant activity and is applicable in Parkinson’s disease research.

BChE-IN-12, also known as compound 12, is a potent non-competitive inhibitor of butyrylcholinesterase (BChE) with an IC50 value of 2.3 μM. Derived from Bletilla striata, it is utilised in research related to Alzheimer's disease (AD) [1].

AChE BChE-IN-4 (BMC-3) is an AChE and BChE dual inhibitor that can cross the BBB, with IC50 values for human AChE (hAChE) and human BChE (hBChE) of 792 nM and 2.2 nM, respectively[1].

AChE BChE BACE-1-IN-1 (Compound 4k) is an orally active inhibitor that targets acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), with IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM against hAChE, hBChE, and hBACE-1, respectively. It exhibits significant binding affinity with PAS-AChE, excellent blood-brain barrier permeability, potential disassembly of amyloid-beta (Aβ) aggregates, neuroprotective properties against Aβ-induced stress, and remarkable antioxidant capabilities [1].

BChE-IN-10 (compound 6), isolated from Bletilla striata, is a potent mixed-type butyrylcholinesterase (BChE) inhibitor exhibiting an IC50 value of 6.4 μM. It is utilized in Alzheimer's disease (AD) research [1].

BChE-IN-20 (compound 7c) is a potent and selective inhibitor of BChE, with IC50 values of 105 nM for eqBChE and 2.3 nM for hBChE. It also inhibits P glycoprotein with an IC50 of 0.27 μM. BChE-IN-20 serves as a promising template for the design and development of pharmaceutical BChE-selective ligands, including inhibitors and fluorogenic probes.

hBChE-IN-2 is a butyrylcholinesterase (BChE) inhibitor and cannabinoid receptor 2 (CB2R) agonist with neuroprotective activity for the study of Alzheimer's disease-like neurological disorders.

Histone acetyltransferase p300 Inhibitor 4c is a 2-aminothiazole derivative. Histone acetyltransferase p300 Inhibitor 4c inhibited hCA I, hCA II, AChE and BChE with Ki values of 0.008 ± 0.001, 0.124 ± 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 µM. 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 μM.

1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.

Rivastigmine (Exelon) is a Cholinesterase Inhibitor, used for therapy of Alzheimer disease.

Ethyl (triphenylphosphoranylidene) acetate ((Carbethoxymethylene)triphenylphosphorane) may act as an cholinesterase inhibitor that inhibits AChE and BChE.

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density volume and mineralization in vivo.

Benactyzine hydrochloride (Neuroleptone) is a centrally acting muscarinic antagonist. Benactyzine has been used in the treatment of depression and is used in research to investigate the role of cholinergic systems on behavior.

hBChE-IN-1 (compound 4), a quinolizidinyl derivative, effectively inhibits human Butyrylcholinesterase (hBChE) with an IC50 value of 7 nM, demonstrating high selectivity against human Acetylcholinesterase (hAChE). It also inhibits tau and Aβ 40 protein aggregation, with IC50 values of 20 and 4.3 μM, respectively, making it valuable for Alzheimer's disease research [1].