Cholinesterase Inhibitors: Structure of Eserine

Structure Based 3D-QSAR Studies on Cholinesterase Inhibitors

Alzheimer’s disease (AD) is a slowly progressive neurodegenerative disorder of the elderly. It is characterized by widespread loss of central cholinergic neuronal function (Butters et al., 1995). The only symptomatic treatment proven to be effective to date is the use of cholinesterase inhibitors (ChEI) to augment surviving cholinergic activity (Giacobini, 2003, Terry & Buccafusco, 2003). Two t...

Cholinesterase inhibitors and memory.

A consensus exists that cholinesterase inhibitors (ChEIs) are efficacious for mild to moderate Alzheimer's Disease (AD). Unfortunately, the number of non-responders is large and the therapeutic effect is usually short-lasting. In experimental animals, ChEIs exert three main actions: inhibit cholinesterase (ChE), increase extracellular levels of brain acetylcholine (ACh), improve cognitive proce...

Two selective inhibitors of cholinesterase.

Half-inhibition concentrations of new cholinesterase inhibitors.

The power of chosen carbamates and hydrazinium derivatives (carbazates) to inhibit the hydrolysis of acetylthiocholine by butyrylcholinesterase or acetylcholinesterase was tested. The determined pI50 values (= negative logarithm of the molar concentration inhibiting the enzyme activity by 50%) of the tested substances were compared with pI50 values of the commercially used drugs for the Alzheim...

Kinetics of 13 new cholinesterase inhibitors.

Kinetics of hydrolysis of acetylcholine and acetylthiocholine by two types of acetylcholinesterase and butyrylcholinesterase inhibited by 13 new inhibitors (5 carbamates and 8 carbazates--hydrazinium derivatives) was measured in vitro in a batch reactor at 25 degrees C, pH 8, ionic strength 0.11 M and enzyme activity 3.5 U by four nondependent analytical methods. Sevin, rivastigmin (Exelon) and...