achein3

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

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.

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.

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-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 a small-molecule acetylcholinesterase inhibitor with an IC50 value of 4.4 μM that demonstrates neuroprotective activity by suppressing intracellular reactive oxygen species accumulation and inhibiting hydrogen peroxide–induced apoptosis, thereby serving as a research compound for Alzheimer’s disease models and oxidative stress–associated neuronal injury studies.

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].

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].