Synthesis of 3-aminocoumarin-N-benzylpyridinium conjugates with nanomolar inhibitory activity against acetylcholinesterase

design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues

Convergent synthesis of arisugacin skeletons and their acetylcholinesterase inhibitory activity.

In the course of our screening of microbial metabolites that inhibit the activity of acetylcholinesterase (AchE), we isolated potent and selective inhibitors of AchE, arisugacin A (1) and B (2) from the culture broth of Penicillium sp. FO-42591~4^ together with the structurally related known compound, territrem B (3) (Fig. 1)5'6). Interestingly, structures 1-3 resemble the pyripyropene A (4), w...

Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues.

Three series (series A-C) of coumarin analogues with phenylpiperazine functions as substitution were designed and synthesized for studying their potential for treating Alzheimer's (AD) disease. Their anticholinesterase activities were assayed according to Ellmann's method against freshly prepared acetylcholinesterase (AChE) from Electrophorus electricus using donepezil as the reference compound...

Acetylcholinesterase Inhibitory Activity of Standardized Cannabinoids-rich Fractions

Background: Since cannabis has been legally allowed for medicinal purposes in many countries, it has become more interesting issue, particularly in neurologic disorders such as Alzheimer’s disease (AD). Inhibition of acetylcholinesterase (AChE) is one of the mechanisms for the treatment of AD. Objectives: The present study aimed to establish a method for preparation of cannabinoids-rich extrac...

Synthesis and acetylcholinesterase inhibitory evaluation of 4-(1,3-Dioxoisoindolin-2-yl)-N-phenylbenzamide derivatives as potential anti-alzheimer agents

Patients with Alzheimer's disease have cognitive deficits, impaired long-term potentiation and learning and memory. A progressive reduction in cholinergic neurons in some areas of the brain such as cortex and hippocampus is related to the deficits in memory and cognitive function in Alzheimer’s disease (AD). In the current project a new series of phthalimide derivatives were synthesized. Phthal...