The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers variable lengths is described. multivalent inhibition potencies for were investigated acetylcholinesterase. Two displayed small but significant potency in which affinity each increased up 3.2 times when they connected scaffold.

Observations with acetylcholinesterase can be well explained by postulating that the active site contains two subsites: one, an anionic site which binds and orients substituted ammonium ions, and the other, an esteratic site where the hydrolytic process occurs and which contains a basic group which is acetylated and deacetylated during the process (4, 5). The formation of an acetyl enzyme sugge...

Acetylcholinesterase hydrolyzes the neurotransmitter called acetylcholine and is crucially involved in the regulation of neurotransmission. One of the observable facts in the neurodegenerative disorders like Alzheimer's disease is the decrease in the level of acetylcholine. Available drugs that are used for the treatment of Alzheimer's disease are primarily acetylcholinesterase inhibitors with ...

INTRODUCTION A treatment to the Alzheimer's disease consists inhibition of the acetylcholinesterase, which is responsible for the acetylcholine control in the synapses. METHODS We have investigated the potential of inhibition of the acetylcholinesterase produced by hexane extracts of leaves, branches, and flowers from three Bauhinia specimens, which is based on the technique of thin layer chr...

Filariasis is a major health problem, affecting millions of people in tropical and subtropical regions of the world. Targeting the parasite specific enzyme is not only rational but essential for developing effective control measure against filariasis. In our earlier studies we have identified two isozymic forms of acetylcholinesterase (AchE) from bovine filarial parasites (Setaria cervi) differ...

Factors such as oxidative stress and reduced acetylcholine level have been implicated in Alzheimer’s disease (AD) pathology and recently there has been a trend towards natural product research to find potential sources of antioxidants and acetylcholinesterase inhibitors in the plants kingdom. Centaurea is a genus with about 500 species world wild, many of them have shown to possess bio...