Cholinesterase and Neurodegenerative Diseases

Tunable nucleofugality in carbamoyl-bearing covalent cholinesterase inhibitors

This study explores carbamoyl warhead reactivity in covalent cholinesterase inhibitors, identifying structure-reactivity relationships and demonstrating a highly selective, irreversible inhibitor.

Pharmacological Reversal of Attention Deficits in Non-Human Primates: Implications for Alzheimer's Disease

This study evaluates attention-enhancing drugs in non-human primates using a pharmacological model of cholinergic dysfunction, finding nicotine effectively restores attentional performance.

Cardiac acetylcholinesterase and butyrylcholinesterase have distinct localization and function

This study investigates the localization and function of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in the heart, revealing distinct roles and responses to inhibitors.

Development of a High-throughput Assay to Identify Novel Reactivators of Acetylcholinesterase

The paper develops a high-throughput assay to test compounds for reactivating acetylcholinesterase inhibited by organophosphates, validated with 42 in silico selected compounds.

Morphing Cholinesterase Inhibitor Amiridine into Multipotent Drugs for the Treatment of Alzheimer's Disease

This study develops multi-target directed ligands (MTDLs) by modifying amiridine, a cholinesterase inhibitor, to enhance its therapeutic potential for Alzheimer's disease.

2D-QSAR and Molecular Docking based virtual screening of the herbal molecules against Alzheimers Disorder: An approach to predict CNS activity

The paper develops a 2D-QSAR model to predict AChE inhibitory activity and BBB penetration of herbal molecules for Alzheimer's treatment, identifying amentoflavone as the most promising candidate.

Neuroprotective derivatives of tacrine that target NMDA receptor and acetyl cholinesterase - Design, synthesis and biological evaluation

The paper designs, synthesizes, and evaluates neuroprotective derivatives of tacrine that target both acetylcholinesterase and NMDA receptors, showing reduced hepatotoxicity and potential therapeutic benefits.

Rescuing the attentional performance of rats with cholinergic losses by the M1 positive allosteric modulator TAK-071

This study shows that TAK-071, an M1 PAM, improves attentional performance in rats with cholinergic losses, particularly in recovery after distractors.

TAK-071, a muscarinic M1 receptor positive allosteric modulator, attenuates scopolamine-induced quantitative electroencephalogram power spectral changes in cynomolgus monkeys

This study evaluates TAK-071's effect on qEEG power bands in cynomolgus monkeys challenged with scopolamine, showing suppression of scopolamine-induced increases in alpha, theta, and delta power bands.

AchE-OGT dual inhibitors: Potential Partners in Handling Alzheimer’s Disease

The paper identifies donepezil as a dual inhibitor of AchE and OGT, revealing structural features that enable interactions with both targets.