Inhibition of acetylcholinesterase (AChE) using small molecules is still one of the most successful therapeutic strategies in the treatment of Alzheimer's disease (AD). Previously we reported compound T5369186 with a core of quinolone as a new cholinesterase inhibitor. In the present study, in order to identify new cores for the designing of AChE inhibitors, we screened different derivatives of...

A wide range of evidence shows that acetylcholinesterase (AChE) inhibitors can interfere with the progression of Alzheimer's disease (AD). The successful development of these compounds was based on a well-accepted theory that the decline in cognitive and mental functions associated with AD is related to the loss of cortical cholinergic neurotransmission. The earliest known AChE inhibitors, name...

The carbamate compounds are a class of cholinesterase-inhibiting pesticides (Farage-Elawar, 1990) and bendiocarb (2, 3-isopropyledene-dioxyphenyl methylcarbamate, BC) is the most widely used carbamate insecticide to control disease vectors (mosquitoes, flies, household and agricultural pests). Like other carbamate insecticides, BC is a reversible inhibitor of acetylcholinesterase (AChE). The bl...

brain disease that occurs in around 10% of the elderly and, as yet, there is no known cure. The most effective treatments are medications that attempt to increase the brain’s levels of acetylcholine, an important neurotransmitter whose levels decrease with onset of disease. These drugs work by interfering with acetylcholine esterase (AChE), an enzyme that breaks down acetylcholine (Fig. 1). Res...

A wide range of evidence show that acetylcholinesterase (AChE) inhibitors can interfere with the progression of Alzheimer's Disease (AD). The successful development of these compounds was based on a well-accepted theory that the decline in cognitive and mental functions associated with AD is related to the loss of cortical cholinergic neurotransmission. The earliest known AChE inhibitors, namel...

Many pesticides used in agriculture have a negative effect on organisms. The group of hazardous pesticides includes the cholinesterase inhibitor bendiocarbamate. According to literature, bendiocarbamate has relatively low toxicity in mammals and vertebrates in general, since it does accumulate in their tissues and the cholinesterase activity returns to norm within 24 h after acute exposure. The...

A series of tacrine-rhein hybrid compounds have been designed and synthesized as novel multifunctional potent ChE inhibitors. Most of the compounds inhibited ChEs in the nanomolar range in vitro effectively. Compound 10b was one of the most potent inhibitors and was 5-fold more active than tacrine toward AChE, and it also showed a moderate BuChE inhibition with an IC50 value of 200 nM. Kinetic ...

Rat pheochromocytoma PC12 cells undergo neuronal differentiation in response to nerve growth factor. We show here that exposure of PC12 cells to Nardostachys chinensis glycoside induces the outgrowth of neurites, increases the activity of AChE, triggers cell cycle arrest in G1 and enhances the expression of growth associated protein 43 (GAP-43). Both the outgrowth of neurites and the increase i...